Literature DB >> 31710718

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Nuclear hormone receptors.

Stephen P H Alexander1, John A Cidlowski2, Eamonn Kelly3, Alistair Mathie4, John A Peters5, Emma L Veale4, Jane F Armstrong6, Elena Faccenda6, Simon D Harding6, Adam J Pawson6, Joanna L Sharman6, Christopher Southan5, Jamie A Davies6.   

Abstract

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14750. Nuclear hormone receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.
© 2019 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of The British Pharmacological Society.

Entities:  

Year:  2019        PMID： 31710718      PMCID： PMC6844575          DOI： 10.1111/bph.14750

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


Conflict of interest

The authors state that there are no conflicts of interest to disclose.

Overview

Nuclear receptors are specialised transcription factors with commonalities of sequence and structure, which bind as homo‐ or heterodimers to specific consensus sequences of DNA (response elements) in the promoter region of particular target genes. They regulate (either promoting or repressing) transcription of these target genes in response to a variety of endogenous ligands. Endogenous agonists are hydrophobic entities which, when bound to the receptor promote conformational changes in the receptor to allow recruitment (or dissociation) of protein partners, generating a large multiprotein complex. Two major subclasses of nuclear receptors with identified endogenous agonists can be identified: steroid and non‐steroid hormone receptors. Steroid hormone receptors function typically as dimeric entities and are thought to be resident outside the nucleus in the unliganded state in a complex with chaperone proteins, which are liberated upon agonist binding. Migration to the nucleus and interaction with other regulators of gene transcription, including RNA polymerase, acetyltransferases and deacetylases, allows gene transcription to be regulated. Non‐steroid hormone receptors typically exhibit a greater distribution in the nucleus in the unliganded state and interact with other nuclear receptors to form heterodimers, as well as with other regulators of gene transcription, leading to changes in gene transcription upon agonist binding. Selectivity of gene regulation is brought about through interaction of nuclear receptors with particular consensus sequences of DNA, which are arranged typically as repeats or inverted palindromes to allow accumulation of multiple transcription factors in the promoter regions of genes.

Family structure

S230 1A. Thyroid hormone receptors S231 1B. Retinoic acid receptors S232 1C. Peroxisome proliferator‐activated receptors S233 1D. Rev‐Erb receptors S234 1F. Retinoic acid‐related orphans S234 1H. Liver X receptor‐like receptors S235 1I. Vitamin D receptor‐like receptors S236 2A. Hepatocyte nuclear factor‐4 receptors S237 2B. Retinoid X receptors S238 2C. Testicular receptors S238 2E. Tailless‐like receptors S239 2F. COUP‐TF‐like receptors S239 3B. Estrogen‐related receptors S240 4A. Nerve growth factor IB‐like receptors S241 5A. Fushi tarazu F1‐like receptors S241 6A. Germ cell nuclear factor receptors S242 0B. DAX‐like receptors S242 Steroid hormone receptors S243 3A. Estrogen receptors S244 3C. 3‐Ketosteroid receptors

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=84

Overview

Thyroid hormone receptors (TRs, nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132849?dopt=AbstractPlus ]) are nuclear hormone receptors of the NR1A family, with diverse roles regulating macronutrient metabolism, cognition and cardiovascular homeostasis. TRs are activated by thyroxine (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2635) and thyroid hormone (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2634). Once activated by a ligand, the receptor acts as a transcription factor either as a monomer, homodimer or heterodimer with members of the retinoid X receptor family. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2633 has been described as an antagonist at TRs with modest selectivity for TRβ [http://www.ncbi.nlm.nih.gov/pubmed/12109914?dopt=AbstractPlus].

Comments

An interaction with integrin αVβ3 has been suggested to underlie plasma membrane localization of TRs and non‐genomic signalling [http://www.ncbi.nlm.nih.gov/pubmed/15802494?dopt=AbstractPlus].One splice variant, TRα2, lacks a functional DNA‐binding domain and appears to act as a transcription suppressor. Although radioligand binding assays have been described for these receptors, the radioligands are not commercially available.

Further reading on 1A. Thyroid hormone receptors

Elbers LP et al. (2016) Thyroid Hormone Mimetics: the Past, Current Status and Future Challenges. Curr Atheroscler Rep 18: 14 https://www.ncbi.nlm.nih.gov/pubmed/26886134?dopt=AbstractPlus Flamant F et al. (2006) International Union of Pharmacology. LIX. The pharmacology and classification of the nuclear receptor superfamily: thyroid hormone receptors. Pharmacol. Rev. 58: 705‐11 https://www.ncbi.nlm.nih.gov/pubmed/17132849?dopt=AbstractPlus Mendoza A et al. (2017) New insights into thyroid hormone action. Pharmacol. Ther. 173: 135‐145 https://www.ncbi.nlm.nih.gov/pubmed/28174093?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=85

Retinoic acid receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132850?dopt=AbstractPlus ]) are nuclear hormone receptors of the NR1B family activated by the vitamin A‐derived agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2644 (ATRA) and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2645, and the RAR‐selective synthetic agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2646 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5429. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2641 is a family‐selective antagonist [http://www.ncbi.nlm.nih.gov/pubmed/19477412?dopt=AbstractPlus]. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2642 has been suggested to be a PPARγ agonist [http://www.ncbi.nlm.nih.gov/pubmed/17290005?dopt=AbstractPlus]. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3433 is an antagonist with selectivity for RARα and RARβ compared with RARγ [http://www.ncbi.nlm.nih.gov/pubmed/10331664?dopt=AbstractPlus].

Further reading on 1B. Retinoic acid receptors

Duong V et al. (2011) The molecular physiology of nuclear retinoic acid receptors. From health to disease. Biochim. Biophys. Acta 1812: 1023‐31 [https://www.ncbi.nlm.nih.gov/pubmed/20970498?dopt=AbstractPlus] Germain P et al. (2006) International Union of Pharmacology. LX. Retinoic acid receptors. Pharmacol. Rev. 58: 712‐25 https://www.ncbi.nlm.nih.gov/pubmed/17132850?dopt=AbstractPlus Larange A et al. (2016) Retinoic Acid and Retinoic Acid Receptors as Pleiotropic Modulators of the Immune System. Annu. Rev. Immunol. 34: 369‐94 https://www.ncbi.nlm.nih.gov/pubmed/27168242?dopt=AbstractPlus Saeed A et al. (2017) The interrelationship between bile acid and vitamin A homeostasis. Biochim. Biophys. Acta 1862: 496‐512 https://www.ncbi.nlm.nih.gov/pubmed/28111285?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=86

Peroxisome proliferator‐activated receptors (PPARs, nomenclature as agreed by the NC‐IUPHAR Subcommittee on Nuclear Hormone Receptors [http://www.ncbi.nlm.nih.gov/pubmed/17132851?dopt=AbstractPlus]) are nuclear hormone receptors of the NR1C family, with diverse roles regulating lipid homeostasis, cellular differentiation, proliferation and the immune response. PPARs have many potential endogenous agonists [http://www.ncbi.nlm.nih.gov/pubmed/12749590?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/17132851?dopt=AbstractPlus], including http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1877, prostacyclin (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1915), many fatty acids and their oxidation products, lysophosphatidic acid (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2906) [http://www.ncbi.nlm.nih.gov/pubmed/12502787?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5426, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3401, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5427, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5428 and leukotriene B4 (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2487). http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2668 acts as a non‐selective agonist for the PPAR family [http://www.ncbi.nlm.nih.gov/pubmed/10691680?dopt=AbstractPlus]. These receptors also bind hypolipidaemic drugs (PPARα) and anti‐diabetic thiazolidinediones (PPARγ), as well as many non‐steroidal anti‐inflammatory drugs, such as http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5425 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1909. Once activated by a ligand, the receptor forms a heterodimer with members of the retinoid X receptor family and can act as a transcription factor. Although radioligand binding assays have been described for all three receptors, the radioligands are not commercially available. Commonly, receptor occupancy studies are conducted using fluorescent ligands and truncated forms of the receptor limited to the ligand binding domain. As with the estrogen receptor antagonists, many agents show tissue‐selective efficacy (e.g. [http://www.ncbi.nlm.nih.gov/pubmed/11030710?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/11991651?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/11684010?dopt=AbstractPlus]). Agonists with mixed activity at PPARα and PPARγ have also been described (e.g [http://www.ncbi.nlm.nih.gov/pubmed/15120604?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/14701675?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/15115385?dopt=AbstractPlus]).

Further reading on 1C. Peroxisome proliferator‐activated receptors

Cheang WS et al. (2015) The peroxisome proliferator‐activated receptors in cardiovascular diseases: experimental benefits and clinical challenges. Br. J. Pharmacol. 172: 5512‐22 [https://www.ncbi.nlm.nih.gov/pubmed/25438608?dopt=AbstractPlus] Gross B et al. (2017) PPARs in obesity‐induced T2DM, dyslipidaemia and NAFLD. Nat Rev Endocrinol 13: 36‐49 [https://www.ncbi.nlm.nih.gov/pubmed/27636730?dopt=AbstractPlus] Hallenborg P et al. (2016) The elusive endogenous adipogenic PPARγ agonists: Lining up the suspects. Prog. Lipid Res. 61: 149‐62 [https://www.ncbi.nlm.nih.gov/pubmed/26703188?dopt=AbstractPlus] Michalik L et al. (2006) International Union of Pharmacology. LXI. Peroxisome proliferator‐activated receptors. Pharmacol. Rev. 58: 726‐41 [https://www.ncbi.nlm.nih.gov/pubmed/17132851?dopt=AbstractPlus] Sauer S. (2015) Ligands for the Nuclear Peroxisome Proliferator‐Activated Receptor Gamma. Trends Pharmacol. Sci. 36: 688‐704 [https://www.ncbi.nlm.nih.gov/pubmed/26435213?dopt=AbstractPlus]

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=87

Rev‐erb receptors (nomenclature as agreed by the NC‐IUPHAR Subcommittee on Nuclear Hormone Receptors [http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus]) have yet to be officially paired with an endogenous ligand, but are thought to be activated by heme.

Further reading on 1D. Rev‐Erb receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 [https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus] Gonzalez‐Sanchez E et al. (2015) Nuclear receptors in acute and chronic cholestasis. Dig Dis 33: 357‐66 [https://www.ncbi.nlm.nih.gov/pubmed/26045270?dopt=AbstractPlus] Gustafson CL et al. (2015) Emerging models for the molecular basis of mammalian circadian timing. Biochemistry 54: 134‐49 [https://www.ncbi.nlm.nih.gov/pubmed/25303119?dopt=AbstractPlus] Sousa EH et al. (2017) Drug discovery targeting heme‐based sensors and their coupled activities. J. Inorg. Biochem. 167: 12‐20 [https://www.ncbi.nlm.nih.gov/pubmed/27893989?dopt=AbstractPlus]

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=88

Retinoic acid receptor‐related orphan receptors (ROR, nomenclature as agreed by the NC‐IUPHAR Subcommittee on Nuclear Hormone Receptors [http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus]) have yet to be assigned a definitive endogenous ligand, although RORα may be synthesized with a ‘captured’ agonist such as http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2718 [http://www.ncbi.nlm.nih.gov/pubmed/14722075?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12467577?dopt=AbstractPlus]. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2644 shows selectivity for RORβ within the ROR family [http://www.ncbi.nlm.nih.gov/pubmed/12958591?dopt=AbstractPlus]. RORα has been suggested to be a nuclear receptor responding to http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=224 [http://www.ncbi.nlm.nih.gov/pubmed/7885826?dopt=AbstractPlus].

Further reading on 1F. Retinoic acid‐related orphans

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 [https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus] Cyr P et al. (2016) Recent progress on nuclear receptor RORγ modulators. Bioorg. Med. Chem. Lett. 26: 4387‐4393 [https://www.ncbi.nlm.nih.gov/pubmed/27542308?dopt=AbstractPlus] Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 [https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus] Guillemot‐Legris O et al. (2016) Oxysterols in Metabolic Syndrome: From Bystander Molecules to Bioactive Lipids. Trends Mol Med 22: 594‐614 [https://www.ncbi.nlm.nih.gov/pubmed/27286741?dopt=AbstractPlus] Mutemberezi V et al. (2016) Oxysterols: From cholesterol metabolites to key mediators. Prog. Lipid Res. 64: 152‐169 [https://www.ncbi.nlm.nih.gov/pubmed/27687912?dopt=AbstractPlus]

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=89

Liver X and farnesoid X receptors (LXR and FXR, nomenclature as agreed by the NC‐IUPHAR Subcommittee on Nuclear Hormone Receptors [http://www.ncbi.nlm.nih.gov/pubmed/17132852?dopt=AbstractPlus]) are members of a steroid analogue‐activated nuclear receptor subfamily, which form heterodimers with members of the retinoid X receptor family. Endogenous ligands for LXRs include hydroxycholesterols (OHC), while FXRs appear to be activated by bile acids. In humans and primates, NR1H5P is a pseudogene. However, in other mammals, it encodes a functional nuclear hormone receptor that appears to be involved in cholesterol biosynthesis [http://www.ncbi.nlm.nih.gov/pubmed/12529392?dopt=AbstractPlus]. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2755 [http://www.ncbi.nlm.nih.gov/pubmed/10968783?dopt=AbstractPlus] and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2754 [http://www.ncbi.nlm.nih.gov/pubmed/11985463?dopt=AbstractPlus] are synthetic agonists acting at both LXRα and LXRβ with less than 10‐fold selectivity.

Further reading on 1H. Liver X receptor‐like receptors

Courtney R et al. (2016) LXR Regulation of Brain Cholesterol: From Development to Disease. Trends Endocrinol. Metab. 27: 404‐414 [https://www.ncbi.nlm.nih.gov/pubmed/27113081?dopt=AbstractPlus] El‐Gendy BEM et al. (2018) Recent Advances in the Medicinal Chemistry of Liver X Receptors. J. Med. Chem. 61: 10935‐10956 [https://www.ncbi.nlm.nih.gov/pubmed/30004226?dopt=AbstractPlus] Gadaleta RM et al. (2010) Bile acids and their nuclear receptor FXR: Relevance for hepatobiliary and gastrointestinal disease. Biochim. Biophys. Acta 1801: 683‐92 [https://www.ncbi.nlm.nih.gov/pubmed/20399894?dopt=AbstractPlus] Merlen G et al. (2017) Bile acids and their receptors during liver regeneration: “Dangerous protectors”. Mol. Aspects Med. 56: 25‐33 [https://www.ncbi.nlm.nih.gov/pubmed/28302491?dopt=AbstractPlus] Moore DD et al. (2006) International Union of Pharmacology. LXII. The NR1H and NR1I receptors: constitutive androstane receptor, pregnene X receptor, farnesoid X receptor alpha, farnesoid X receptor beta, liver X receptor alpha, liver X receptor beta, and vitamin D receptor. Pharmacol. Rev. 58: 742‐59 [https://www.ncbi.nlm.nih.gov/pubmed/17132852?dopt=AbstractPlus] Mouzat K et al. (2016) Liver X receptors: from cholesterol regulation to neuroprotection‐a new barrier against neurodegeneration in amyotrophic lateral sclerosis? Cell. Mol. Life Sci. 73: 3801‐8 [https://www.ncbi.nlm.nih.gov/pubmed/27510420?dopt=AbstractPlus] Schulman IG. (2017) Liver X receptors link lipid metabolism and inflammation. FEBS Lett. 591: 2978‐2991 [https://www.ncbi.nlm.nih.gov/pubmed/28555747?dopt=AbstractPlus]

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=90

Vitamin D (VDR), Pregnane X (PXR) and Constitutive Androstane (CAR) receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132852?dopt=AbstractPlus ]) are members of the NR1I family of nuclear receptors, which form heterodimers with members of the retinoid X receptor family. PXR and CAR are activated by a range of exogenous compounds, with no established endogenous physiological agonists, although high concentrations of bile acids and bile pigments activate PXR and CAR [http://www.ncbi.nlm.nih.gov/pubmed/17132852?dopt=AbstractPlus].

Further reading on 1I. Vitamin D receptor‐like receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Long MD et al. (2015) Vitamin D receptor and RXR in the post‐genomic era. J. Cell. Physiol. 230: 758‐66 https://www.ncbi.nlm.nih.gov/pubmed/25335912?dopt=AbstractPlus Moore DD et al. (2006) International Union of Pharmacology. LXII. The NR1H and NR1I receptors: constitutive androstane receptor, pregnene X receptor, farnesoid X receptor alpha, farnesoid X receptor beta, liver X receptor alpha, liver X receptor beta, and vitamin D receptor. Pharmacol. Rev. 58: 742‐59 https://www.ncbi.nlm.nih.gov/pubmed/17132852?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=91

The nomenclature of hepatocyte nuclear factor‐4 receptors is agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]. While linoleic acid has been identified as the endogenous ligand for HNF4α its function remains ambiguous [http://www.ncbi.nlm.nih.gov/pubmed/19440305?dopt=AbstractPlus]. HNF4γ has yet to be paired with an endogenous ligand.

Further reading on 2A. Hepatocyte nuclear factor‐4 receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Garattini E et al. (2016) Lipid‐sensors, enigmatic‐orphan and orphan nuclear receptors as therapeutic targets in breast‐cancer. Oncotarget 7: 42661‐42682 https://www.ncbi.nlm.nih.gov/pubmed/26894976?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Lu H. (2016) Crosstalk of HNF4α with extracellular and intracellular signaling pathways in the regulation of hepatic metabolism of drugs and lipids. Acta Pharm Sin B 6: 393‐408 https://www.ncbi.nlm.nih.gov/pubmed/27709008?dopt=AbstractPlus Walesky C et al. (2015) Role of hepatocyte nuclear factor 4α (HNF4α) in cell proliferation and cancer. Gene Expr. 16: 101‐8 https://www.ncbi.nlm.nih.gov/pubmed/25700366?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=92

Retinoid X receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132853?dopt=AbstractPlus ]) are NR2B family members activated by http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2645 and the RXR‐selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2807 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2808, sometimes referred to as rexinoids. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2816 [http://www.ncbi.nlm.nih.gov/pubmed/17947383?dopt=AbstractPlus] and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8079 [http://www.ncbi.nlm.nih.gov/pubmed/10748721?dopt=AbstractPlus] have been described as a pan‐RXR antagonists. These receptors form RXR‐RAR heterodimers and RXR‐RXR homodimers [http://www.ncbi.nlm.nih.gov/pubmed/8801176?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/8521508?dopt=AbstractPlus].

Further reading on 2B. Retinoid X receptors

Germain P et al. (2006) International Union of Pharmacology. LXIII. Retinoid X receptors. Pharmacol. Rev. 58: 760‐72 https://www.ncbi.nlm.nih.gov/pubmed/17132853?dopt=AbstractPlus Long MD et al. (2015) Vitamin D receptor and RXR in the post‐genomic era. J. Cell. Physiol. 230: 758‐66 https://www.ncbi.nlm.nih.gov/pubmed/25335912?dopt=AbstractPlus Menéndez‐Gutiérrez MP et al. (2017) The multi‐faceted role of retinoid X receptor in bone remodeling. Cell. Mol. Life Sci. 74: 2135‐2149 https://www.ncbi.nlm.nih.gov/pubmed/28105491?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=93

Testicular receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand, although testicular receptor 4 has been reported to respond to retinoids.

Further reading on 2C. Testicular receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Safe S et al. (2014) Minireview: role of orphan nuclear receptors in cancer and potential as drug targets. Mol. Endocrinol. 28: 157‐72 https://www.ncbi.nlm.nih.gov/pubmed/24295738?dopt=AbstractPlus Wu D et al. (2016) The emerging roles of orphan nuclear receptors in prostate cancer. Biochim. Biophys. Acta 1866: 23‐36 https://www.ncbi.nlm.nih.gov/pubmed/27264242?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=94

Tailless‐like receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand.

Further reading on 2E. Tailless‐like receptors

Benod C et al. (2016) TLX: An elusive receptor. J. Steroid Biochem. Mol. Biol. 157: 41‐7 https://www.ncbi.nlm.nih.gov/pubmed/26554934?dopt=AbstractPlus Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus O’Leary JD et al. (2018) Regulation of behaviour by the nuclear receptor TLX. Genes Brain Behav. 17: e12357 https://www.ncbi.nlm.nih.gov/pubmed/27790850?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=95

COUP‐TF‐like receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand.

Further reading on 2F. COUP‐TF‐like receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Wu D et al. (2016) The emerging roles of orphan nuclear receptors in prostate cancer. Biochim. Biophys. Acta 1866: 23‐36 https://www.ncbi.nlm.nih.gov/pubmed/27264242?dopt=AbstractPlus Wu SP etal. (2016) Choose your destiny: Make a cell fate decision with COUP‐TFII. J. Steroid Biochem. Mol. Biol. 157: 7‐12 https://www.ncbi.nlm.nih.gov/pubmed/26658017?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=97

Estrogen‐related receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand.

Further reading on 3B. Estrogen‐related receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Divekar SD et al. (2016) Estrogen‐related receptor β (ERRβ) ‐ renaissance receptor or receptor renaissance? Nucl Recept Signal 14: e002 https://www.ncbi.nlm.nih.gov/pubmed/27507929?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Tam IS et al. (2016) There and back again: The journey of the estrogen‐related receptors in the cancer realm. J. Steroid Biochem. Mol. Biol. 157: 13‐9 https://www.ncbi.nlm.nih.gov/pubmed/26151739?dopt=AbstractPlus Wu D et al. (2016) The emerging roles of orphan nuclear receptors in prostate cancer. Biochim. Biophys. Acta 1866: 23‐36 https://www.ncbi.nlm.nih.gov/pubmed/27264242?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=99

Nerve growth factor IB‐like receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand.

Further reading on 4A. Nerve growth factor IB‐like receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Germain Petal. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Ranhotra HS. (2015) The NR4A orphan nuclear receptors: mediators in metabolism and diseases. J. Recept. Signal Transduct. Res. 35: 184‐8 https://www.ncbi.nlm.nih.gov/pubmed/25089663?dopt=AbstractPlus Rodríguez‐Calvo R et al. (2017) The NR4A subfamily of nuclear receptors: potential new therapeutic targets for the treatment of inflammatory diseases. Expert Opin. Ther. Targets 21: 291‐304 https://www.ncbi.nlm.nih.gov/pubmed/28055275?dopt=AbstractPlus Safe S et al. (2016) Nuclear receptor 4A (NR4A) family ‐ orphans no more. J. Steroid Biochem. Mol. Biol. 157: 48‐60 https://www.ncbi.nlm.nih.gov/pubmed/25917081?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=100

Fushi tarazu F1‐like receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand.

Further reading on 5A. Fushi tarazu F1‐like receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Garattini E et al. (2016) Lipid‐sensors, enigmatic‐orphan and orphan nuclear receptors as therapeutic targets in breast‐cancer. Oncotarget 7: 42661‐42682 https://www.ncbi.nlm.nih.gov/pubmed/26894976?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Zhi X et al. (2016) Structures and regulation of non‐X orphan nuclear receptors: A retinoid hypothesis. J. Steroid Biochem. Mol. Biol. 157: 27‐40 https://www.ncbi.nlm.nih.gov/pubmed/26159912?dopt=AbstractPlus Zimmer V et al. (2015) Nuclear receptor variants in liver disease. Dig Dis 33: 415‐9 https://www.ncbi.nlm.nih.gov/pubmed/26045277?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=101

Germ cell nuclear factor receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand.

Further reading on 6A. Germ cell nuclear factor receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Garattini E et al. (2016) Lipid‐sensors, enigmatic‐orphan and orphan nuclear receptors as therapeutic in breast‐cancer. Oncotarget 7: 42661‐42682 https://www.ncbi.nlm.nih.gov/pubmed/26894976?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Safe S et al. (2014) Minireview: role of orphan nuclear receptors in cancer and potential as drug Mol. Endocrinol. 28: 157‐72 https://www.ncbi.nlm.nih.gov/pubmed/24295738?dopt=AbstractPlus Zhi X et al. (2016) Structures and regulation of non‐X orphan nuclear receptors: A retinoid hypothesis. J. Steroid Biochem. Mol. Biol. 157: 27‐40 https://www.ncbi.nlm.nih.gov/pubmed/26159912?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=102

Dax‐like receptors (nomenclature as agreed by the NC‐IUPHAR Subcommittee on Nuclear Hormone Receptors [ http://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus ]) have yet to be officially paired with an endogenous ligand.

Further reading on 0B. DAX‐like receptors

Benoit G et al. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol. Rev. 58: 798‐836 https://www.ncbi.nlm.nih.gov/pubmed/17132856?dopt=AbstractPlus Garattini E et al. (2016) Lipid‐sensors, enigmatic‐orphan and orphan nuclear receptors as therapeutic targets in breast‐cancer. Oncotarget 7: 42661‐42682 https://www.ncbi.nlm.nih.gov/pubmed/26894976?dopt=AbstractPlus Germain P et al. (2006) Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 58: 685‐704 https://www.ncbi.nlm.nih.gov/pubmed/17132848?dopt=AbstractPlus Safe S et al. (2014) Minireview: role of orphan nuclear receptors in cancer and potential as drug targets. Mol. Endocrinol. 28: 157‐72 https://www.ncbi.nlm.nih.gov/pubmed/24295738?dopt=AbstractPlus Wu D et al. (2016) The emerging roles of orphan nuclear receptors in prostate cancer. Biochim. Biophys. Acta 1866: 23‐36 https://www.ncbi.nlm.nih.gov/pubmed/27264242?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=107

Steroid hormone receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132854?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/17132855?dopt=AbstractPlus ]) are nuclear hormone receptors of the NR3 class, with endogenous agonists that may be divided into 3‐hydroxysteroids (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2818 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1013) and 3‐ketosteroids (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2856 [DHT], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2872, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2868, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2869, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2377 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2858). These receptors exist as dimers coupled with chaperone molecules (such as http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5365 (https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:5258, http://www.uniprot.org/uniprot/P08238) and immunophilin FKBP52:https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:3720, http://www.uniprot.org/uniprot/Q02790), which are shed on binding the steroid hormone. Although rapid signalling phenomena are observed [http://www.ncbi.nlm.nih.gov/pubmed/18784332?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/19389460?dopt=AbstractPlus], the principal signalling cascade appears to involve binding of the activated receptors to nuclear hormone response elements of the genome, with a 15‐nucleotide consensus sequence AGAACAnnnTGTTCT (i.e. an inverted palindrome) as homo‐ or heterodimers. They also affect transcription by protein‐protein interactions with other transcription factors, such as activator protein 1 (AP‐1) and nuclear factor B (NF‐B). Splice variants of each of these receptors can form functional or non‐functional monomers that can dimerize to form functional or non‐functional receptors. For example, alternative splicing of PR mRNA produces A and B monomers that combine to produce functional AA, AB and BB receptors with distinct characteristics [http://www.ncbi.nlm.nih.gov/pubmed/8264658?dopt=AbstractPlus]. A 7TM receptor responsive to estrogen (https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:4485, http://www.uniprot.org/uniprot/Q99527, also known as GPR30, see [http://www.ncbi.nlm.nih.gov/pubmed/18271749?dopt=AbstractPlus]) has been described. Human orthologues of 7TM ’membrane progestin receptors’ (https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:23146, https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:15708 and https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:29645), initially discovered in fish [http://www.ncbi.nlm.nih.gov/pubmed/12601167?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12574519?dopt=AbstractPlus], appear to localize to intracellular membranes and respond to ’non‐genomic’ progesterone analogues independently of G proteins [http://www.ncbi.nlm.nih.gov/pubmed/18603275?dopt=AbstractPlus].

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=96

Estrogen receptor (ER) activity regulates diverse physiological processes via transcriptional modulation of target genes. The selection of target genes and the magnitude of the response, be it induction or repression, are determined by many factors, including the effect of the hormone ligand and DNA binding on ER structural conformation, and the local cellular regulatory environment. The cellular environment defines the specific complement of DNA enhancer and promoter elements present and the availability of coregulators to form functional transcription complexes. Together, these determinants control the resulting biological response. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2822 exhibits partial agonist activity at ERα [http://www.ncbi.nlm.nih.gov/pubmed/10395487?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9927308?dopt=AbstractPlus]. Estrogen receptors may be blocked non‐selectively by http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1016 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2820 and labelled by http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1012 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5384. Many agents thought initially to be antagonists at estrogen receptors appear to have tissue‐specific efficacy (e.g. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1016 is an antagonist at estrogen receptors in the breast, but is an agonist at estrogen receptors in the uterus), hence the descriptor SERM (selective estrogen receptor modulator) or SnuRM (selective nuclear receptor modulator). http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5430 has been suggested to be an ERα‐selective estrogen receptor modulator [http://www.ncbi.nlm.nih.gov/pubmed/17115070?dopt=AbstractPlus].

Further reading on 3A. Estrogen receptors

Coons LA et al. (2017) DNA Sequence Constraints Define Functionally Active Steroid Nuclear Receptor Binding Sites in Chromatin. Endocrinology 158: 3212‐3234 https://www.ncbi.nlm.nih.gov/pubmed/28977594?dopt=AbstractPlus Dahlman‐Wright K et al. (2006) International Union of Pharmacology. LXIV. Estrogen receptors. Pharmacol. Rev. 58: 773‐81 https://www.ncbi.nlm.nih.gov/pubmed/17132854?dopt=AbstractPlus Gonzalez‐Sanchez E et al. (2015) Nuclear receptors in acute and chronic cholestasis. Dig Dis 33: 357‐66 https://www.ncbi.nlm.nih.gov/pubmed/26045270?dopt=AbstractPlus Hewitt SC et al. (2016) What’s new in estrogen receptor action in the female reproductive tract. J. Mol. Endocrinol. 56: R55‐71 https://www.ncbi.nlm.nih.gov/pubmed/26826253?dopt=AbstractPlus Jameera Begam A et al. (2017) Estrogen receptor agonists/antagonists in breast cancer therapy: A critical review. Bioorg. Chem. 71: 257‐274 https://www.ncbi.nlm.nih.gov/pubmed/28274582?dopt=AbstractPlus Warner M et al. (2017) Estrogen Receptor β as a Pharmaceutical Target. Trends Pharmacol. Sci. 38: 92‐99 https://www.ncbi.nlm.nih.gov/pubmed/27979317?dopt=AbstractPlus

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=98

Steroid hormone receptors (nomenclature as agreed by the http://www.ncbi.nlm.nih.gov/pubmed/17132854?dopt=AbstractPlus, https://www.ncbi.nlm.nih.gov/pubmed/17132855?dopt=AbstractPlus ]) are nuclear hormone receptors of the NR3 class, with endogenous agonists that may be divided into 3‐hydroxysteroids (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2818 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1013) and 3‐ketosteroids (http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2856 [DHT], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2872, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2868, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2869, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2377 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2858). http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3447 also binds to MRin vitro. PR antagonists have been suggested to subdivide into Type I (e.g. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2882) and Type II (e.g. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3448) groups. These groups appear to promote binding of PR to DNA with different efficacies and evoke distinct conformational changes in the receptor, leading to a transcription‐neutral complex [http://www.ncbi.nlm.nih.gov/pubmed/9528977?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9849965?dopt=AbstractPlus]. Mutations in AR underlie testicular feminization and androgen insensitivity syndromes, spinal and bulbar muscular atrophy (Kennedy’s disease).

Further reading on 3C. 3‐Ketosteroid receptors

Baker ME et al. (2017) 30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Evolution of the mineralocorticoid receptor: sequence, structure and function. J. Endocrinol. 234: T1‐T16 https://www.ncbi.nlm.nih.gov/pubmed/28468932?dopt=AbstractPlus Carroll JS et al. (2017) Deciphering the divergent roles of progestogens in breast cancer. Nat. Rev. Cancer 17: 54‐64 https://www.ncbi.nlm.nih.gov/pubmed/27885264?dopt=AbstractPlus Cohen DM et al. (2017) Nuclear Receptor Function through Genomics: Lessons from the Glucocorticoid Receptor. Trends Endocrinol. Metab. 28: 531‐540 https://www.ncbi.nlm.nih.gov/pubmed/28495406?dopt=AbstractPlus de Kloet ER et al. (2017) Brain mineralocorticoid receptor function in control of salt balance and stress‐adaptation. Physiol. Behav. 178: 13‐20 https://www.ncbi.nlm.nih.gov/pubmed/28089704?dopt=AbstractPlus Garg D et al. (2017) Progesterone‐Mediated Non‐Classical Signaling. Trends Endocrinol. Metab. 28: 656‐668 https://www.ncbi.nlm.nih.gov/pubmed/28651856?dopt=AbstractPlus Lu NZ et al. (2006) International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors. Pharmacol. Rev. 58: 782‐97 https://www.ncbi.nlm.nih.gov/pubmed/17132855?dopt=AbstractPlus Lucas‐Herald AK et al. (2017) Genomic and non‐genomic effects of androgens in the cardiovascular system: clinical implications. Clin. Sci. 131: 1405‐1418 https://www.ncbi.nlm.nih.gov/pubmed/28645930?dopt=AbstractPlus Wadosky KM et al. (2017) Androgen receptor splice variants and prostate cancer: From bench to bedside. Oncotarget 8: 18550‐18576 https://www.ncbi.nlm.nih.gov/pubmed/28077788?dopt=AbstractPlus Weikum ER et al. (2017) Glucocorticoid receptor control of transcription: precision and plasticity via allostery. Nat. Rev. Mol. Cell Biol. 18: 159‐174 https://www.ncbi.nlm.nih.gov/pubmed/28053348?dopt=AbstractPlus
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=588 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=589
Systematic nomenclatureNR1A1NR1A2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:11796, http://www.uniprot.org/uniprot/P10827 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:11799, http://www.uniprot.org/uniprot/P10828
Rank order of potency http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2634 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2635 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2634 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2635
Agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6951 [http://www.ncbi.nlm.nih.gov/pubmed/6777394?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6951 [http://www.ncbi.nlm.nih.gov/pubmed/6777394?dopt=AbstractPlus]
Selective agonists– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2639 [http://www.ncbi.nlm.nih.gov/pubmed/9653548?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/269396?dopt=AbstractPlus]
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=590 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=591 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=592
Systematic nomenclatureNR1B1NR1B2NR1B3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:9864, http://www.uniprot.org/uniprot/P10276 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:9865, http://www.uniprot.org/uniprot/P10826 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:9866, http://www.uniprot.org/uniprot/P13631
Agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2644 [http://www.ncbi.nlm.nih.gov/pubmed/19058965?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2644 [http://www.ncbi.nlm.nih.gov/pubmed/19058965?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2644 [http://www.ncbi.nlm.nih.gov/pubmed/19058965?dopt=AbstractPlus]
Sub/family‐selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6952 [http://www.ncbi.nlm.nih.gov/pubmed/19058965?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6952 [http://www.ncbi.nlm.nih.gov/pubmed/19058965?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5429 [http://www.ncbi.nlm.nih.gov/pubmed/8544175?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6952 [http://www.ncbi.nlm.nih.gov/pubmed/19058965?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5429 [http://www.ncbi.nlm.nih.gov/pubmed/8544175?dopt=AbstractPlus]
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2650 [http://www.ncbi.nlm.nih.gov/pubmed/10421757?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2648 [http://www.ncbi.nlm.nih.gov/pubmed/20925433?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2647 [http://www.ncbi.nlm.nih.gov/pubmed/1656191?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4054 [http://www.ncbi.nlm.nih.gov/pubmed/16302793?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4055 [http://www.ncbi.nlm.nih.gov/pubmed/19239230?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/16302793?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3431 [http://www.ncbi.nlm.nih.gov/pubmed/8544175?dopt=AbstractPlus]
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2642 (pIC50 6.3–7.2) [http://www.ncbi.nlm.nih.gov/pubmed/1323127?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/8264595?dopt=AbstractPlus]– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4062 [http://www.ncbi.nlm.nih.gov/pubmed/10723137?dopt=AbstractPlus]
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=593 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=594 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=595
Systematic nomenclatureNR1C1NR1C2NR1C3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:9232, http://www.uniprot.org/uniprot/Q07869 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:9235, http://www.uniprot.org/uniprot/Q03181 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:9236, http://www.uniprot.org/uniprot/P37231
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2674 [http://www.ncbi.nlm.nih.gov/pubmed/10389847?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/11354382?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6691 [http://www.ncbi.nlm.nih.gov/pubmed/18971326?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2666 [http://www.ncbi.nlm.nih.gov/pubmed/10691680?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3439 [http://www.ncbi.nlm.nih.gov/pubmed/21889235?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2686 [http://www.ncbi.nlm.nih.gov/pubmed/15939051?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12699745?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2687 [http://www.ncbi.nlm.nih.gov/pubmed/11309497?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2703 [http://www.ncbi.nlm.nih.gov/pubmed/10389847?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2717 (Partial agonist) [http://www.ncbi.nlm.nih.gov/pubmed/11043571?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1056 [http://www.ncbi.nlm.nih.gov/pubmed/9836620?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9013583?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9454824?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2693 [http://www.ncbi.nlm.nih.gov/pubmed/9836620?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9454824?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2694 [http://www.ncbi.nlm.nih.gov/pubmed/9836620?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/11095972?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9454824?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2711 [http://www.ncbi.nlm.nih.gov/pubmed/9836620?dopt=AbstractPlus]
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3440 (pIC50 6.6) [http://www.ncbi.nlm.nih.gov/pubmed/11845213?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3441 (pIC50 6.5) [http://www.ncbi.nlm.nih.gov/pubmed/17975020?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3444 (pK i 9) [http://www.ncbi.nlm.nih.gov/pubmed/11877444?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3442 (Irreversible inhibition) (pIC50 8.1) [http://www.ncbi.nlm.nih.gov/pubmed/12022867?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3443 (pK i 6.9) [http://www.ncbi.nlm.nih.gov/pubmed/11043571?dopt=AbstractPlus]
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=596 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=597
Systematic nomenclatureNR1D1NR1D2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7962, http://www.uniprot.org/uniprot/P20393 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7963, http://www.uniprot.org/uniprot/Q14995
Endogenous agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4349 [http://www.ncbi.nlm.nih.gov/pubmed/18037887?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/18006707?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4349 [http://www.ncbi.nlm.nih.gov/pubmed/24872411?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/18037887?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/18006707?dopt=AbstractPlus]
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2903 [http://www.ncbi.nlm.nih.gov/pubmed/20677822?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2903 [http://www.ncbi.nlm.nih.gov/pubmed/21043485?dopt=AbstractPlus]–
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2904 (pIC50 6.5) [http://www.ncbi.nlm.nih.gov/pubmed/21043485?dopt=AbstractPlus]–
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=598 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=599 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=600
Systematic nomenclatureNR1F1NR1F2NR1F3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10258, http://www.uniprot.org/uniprot/P35398 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10259, http://www.uniprot.org/uniprot/Q92753 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10260, http://www.uniprot.org/uniprot/P51449
Endogenous agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2718 [http://www.ncbi.nlm.nih.gov/pubmed/12467577?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/8858107?dopt=AbstractPlus]––
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3432 [http://www.ncbi.nlm.nih.gov/pubmed/14622968?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2738 [http://www.ncbi.nlm.nih.gov/pubmed/14622968?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12467577?dopt=AbstractPlus]––
Comments––The immune system function of RORC proteins most likely resides with expression of the RORγt isoform by immature CD4+/CD8+ cells in the thymus [http://www.ncbi.nlm.nih.gov/pubmed/15247480?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10875923?dopt=AbstractPlus] and in lymphoid tissue inducer (LTi) cells [http://www.ncbi.nlm.nih.gov/pubmed/14691482?dopt=AbstractPlus].
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=603 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=604 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=602 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=601
Systematic nomenclatureNR1H4NR1H5NR1H3NR1H2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7967, http://www.uniprot.org/uniprot/Q96RI1 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:32673, – https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7966, http://www.uniprot.org/uniprot/Q13133 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7965, http://www.uniprot.org/uniprot/P55055
Potency order http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=608 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=611, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=610 [http://www.ncbi.nlm.nih.gov/pubmed/10334992?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10334993?dopt=AbstractPlus]– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3434, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2742, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2750 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2885, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2752 [http://www.ncbi.nlm.nih.gov/pubmed/9013544?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3434, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2742, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2750 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2885, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2752 [http://www.ncbi.nlm.nih.gov/pubmed/9013544?dopt=AbstractPlus]
Endogenous agonists– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2746 [http://www.ncbi.nlm.nih.gov/pubmed/12529392?dopt=AbstractPlus] – Mouse––
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2743 [http://www.ncbi.nlm.nih.gov/pubmed/10956205?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3435 [http://www.ncbi.nlm.nih.gov/pubmed/12166927?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2744 [http://www.ncbi.nlm.nih.gov/pubmed/12718892?dopt=AbstractPlus]–––
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2745 (pIC50 5.7–6) [http://www.ncbi.nlm.nih.gov/pubmed/12089353?dopt=AbstractPlus]–––
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=605 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=606 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=607
Systematic nomenclatureNR1I1NR1I2NR1I3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12679, http://www.uniprot.org/uniprot/P11473 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7968, http://www.uniprot.org/uniprot/O75469 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7969, http://www.uniprot.org/uniprot/Q14994
Endogenous agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2779 [http://www.ncbi.nlm.nih.gov/pubmed/7976510?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12089348?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1013 [http://www.ncbi.nlm.nih.gov/pubmed/10628745?dopt=AbstractPlus]–
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2777 [http://www.ncbi.nlm.nih.gov/pubmed/1472092?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/8573413?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2790 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2764 [http://www.ncbi.nlm.nih.gov/pubmed/10852961?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10974665?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2759 [http://www.ncbi.nlm.nih.gov/pubmed/10628745?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2739 [http://www.ncbi.nlm.nih.gov/pubmed/9727070?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2765 [http://www.ncbi.nlm.nih.gov/pubmed/9784494?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9727070?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2756 [http://www.ncbi.nlm.nih.gov/pubmed/10757780?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2758 [http://www.ncbi.nlm.nih.gov/pubmed/12611900?dopt=AbstractPlus]
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2788 (pIC50 8.2) [http://www.ncbi.nlm.nih.gov/pubmed/17125259?dopt=AbstractPlus] – Chicken, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2789 (pIC50 7.5) [http://www.ncbi.nlm.nih.gov/pubmed/12901907?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/11094341?dopt=AbstractPlus]––
Comments–– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2330 [http://www.ncbi.nlm.nih.gov/pubmed/10748001?dopt=AbstractPlus] and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2755 [http://www.ncbi.nlm.nih.gov/pubmed/23665929?dopt=AbstractPlus] although acting at other sites, function as antagonists of the constitutive androstane receptor.
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=608 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=609
Systematic nomenclatureNR2A1NR2A2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:5024, http://www.uniprot.org/uniprot/P41235 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:5026, http://www.uniprot.org/uniprot/Q14541
Endogenous agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1052 [http://www.ncbi.nlm.nih.gov/pubmed/19440305?dopt=AbstractPlus]–
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6695 [http://www.ncbi.nlm.nih.gov/pubmed/22840769?dopt=AbstractPlus]–
CommentsHNF4α has constitutive transactivation activity [http://www.ncbi.nlm.nih.gov/pubmed/19440305?dopt=AbstractPlus] and binds DNA as a homodimer [http://www.ncbi.nlm.nih.gov/pubmed/7651430?dopt=AbstractPlus].–
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=610 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=611 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=612
Systematic nomenclatureNR2B1NR2B2NR2B3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10477, http://www.uniprot.org/uniprot/P19793 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10478, http://www.uniprot.org/uniprot/P28702 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10479, http://www.uniprot.org/uniprot/P48443
Sub/family‐selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2807 [http://www.ncbi.nlm.nih.gov/pubmed/8071941?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10052980?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10637371?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2807 [http://www.ncbi.nlm.nih.gov/pubmed/8071941?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10052980?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10637371?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2807 [http://www.ncbi.nlm.nih.gov/pubmed/8071941?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10052980?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/10637371?dopt=AbstractPlus]
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2810 [http://www.ncbi.nlm.nih.gov/pubmed/11805839?dopt=AbstractPlus]––
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=613 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=614
Systematic nomenclatureNR2C1NR2C2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7971, http://www.uniprot.org/uniprot/P13056 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7972, http://www.uniprot.org/uniprot/P49116
Endogenous agonists– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4053 [http://www.ncbi.nlm.nih.gov/pubmed/21068381?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2644 [http://www.ncbi.nlm.nih.gov/pubmed/21068381?dopt=AbstractPlus]
CommentsForms a heterodimer with TR4; gene disruption appears without effect on testicular development or function [http://www.ncbi.nlm.nih.gov/pubmed/12052874?dopt=AbstractPlus].Forms a heterodimer with TR2.
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=615 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=616
Systematic nomenclatureNR2E1NR2E3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7973, http://www.uniprot.org/uniprot/Q9Y466 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7974, http://www.uniprot.org/uniprot/Q9Y5X4
CommentsGene disruption is associated with abnormal brain development [http://www.ncbi.nlm.nih.gov/pubmed/12902391?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9394001?dopt=AbstractPlus].–
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=617 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=618 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=619
Systematic nomenclatureNR2F1NR2F2NR2F6
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7975, http://www.uniprot.org/uniprot/P10589 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7976, http://www.uniprot.org/uniprot/P24468 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7977, http://www.uniprot.org/uniprot/P10588
CommentsGene disruption is perinatally lethal [http://www.ncbi.nlm.nih.gov/pubmed/9271116?dopt=AbstractPlus].Gene disruption is embryonically lethal [http://www.ncbi.nlm.nih.gov/pubmed/10215630?dopt=AbstractPlus].Gene disruption impairs CNS development [http://www.ncbi.nlm.nih.gov/pubmed/15741322?dopt=AbstractPlus].
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=622 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=623 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=624
Systematic nomenclatureNR3B1NR3B2NR3B3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:3471, http://www.uniprot.org/uniprot/P11474 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:3473, http://www.uniprot.org/uniprot/O95718 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:3474, http://www.uniprot.org/uniprot/P62508
CommentsActivated by some dietary flavonoids [http://www.ncbi.nlm.nih.gov/pubmed/14638870?dopt=AbstractPlus]; activated by the synthetic agonist http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2835 [http://www.ncbi.nlm.nih.gov/pubmed/15857113?dopt=AbstractPlus] and blocked by http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2832 [http://www.ncbi.nlm.nih.gov/pubmed/15184675?dopt=AbstractPlus].Maybe activated by http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2834 [http://www.ncbi.nlm.nih.gov/pubmed/15713377?dopt=AbstractPlus].Maybe activated by http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2834 [http://www.ncbi.nlm.nih.gov/pubmed/15713377?dopt=AbstractPlus].
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=629 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=630 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=631
Systematic nomenclatureNR4A1NR4A2NR4A3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7980, http://www.uniprot.org/uniprot/P22736 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7981, http://www.uniprot.org/uniprot/P43354 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7982, http://www.uniprot.org/uniprot/Q92570
CommentsAn endogenous agonist, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5424, has been described [http://www.ncbi.nlm.nih.gov/pubmed/18690216?dopt=AbstractPlus], although structural analysis and molecular modelling has not identified a ligand binding site [http://www.ncbi.nlm.nih.gov/pubmed/12809604?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/15716272?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12774125?dopt=AbstractPlus].––
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=632 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=633
Systematic nomenclatureNR5A1NR5A2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7983, http://www.uniprot.org/uniprot/Q13285 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7984, http://www.uniprot.org/uniprot/O00482
CommentsReported to be inhibited by http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5422 [http://www.ncbi.nlm.nih.gov/pubmed/18055761?dopt=AbstractPlus] and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5423 [http://www.ncbi.nlm.nih.gov/pubmed/18334597?dopt=AbstractPlus].–
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=634
Systematic nomenclatureNR6A1
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7985, http://www.uniprot.org/uniprot/Q15406
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=635 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=636
Systematic nomenclatureNR0B1NR0B2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7960, http://www.uniprot.org/uniprot/P51843 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7961, http://www.uniprot.org/uniprot/Q15466
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=620 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=621
Systematic nomenclatureNR3A1NR3A2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:3467, http://www.uniprot.org/uniprot/P03372 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:3468, http://www.uniprot.org/uniprot/Q92731
Endogenous agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2821 [http://www.ncbi.nlm.nih.gov/pubmed/9048584?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2818 [http://www.ncbi.nlm.nih.gov/pubmed/9048584?dopt=AbstractPlus]–
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2819 [http://www.ncbi.nlm.nih.gov/pubmed/11014206?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/11150164?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7071 [http://www.ncbi.nlm.nih.gov/pubmed/16722623?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4052 [http://www.ncbi.nlm.nih.gov/pubmed/15456246?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2825 [http://www.ncbi.nlm.nih.gov/pubmed/11708925?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/11150164?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6700 [http://www.ncbi.nlm.nih.gov/pubmed/18097065?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/15456246?dopt=AbstractPlus]
Sub/family‐selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7355 (pIC50 7.6) [http://www.ncbi.nlm.nih.gov/pubmed/11356100?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7355 (pIC50 7.1) [http://www.ncbi.nlm.nih.gov/pubmed/11356100?dopt=AbstractPlus]
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4159 (pK i 8.9) [2], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3459 (pK i 8.6) [http://www.ncbi.nlm.nih.gov/pubmed/11861516?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2822 (pK i 8.4) [http://www.ncbi.nlm.nih.gov/pubmed/10395487?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/9927308?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3461 (pK i 6.9) [http://www.ncbi.nlm.nih.gov/pubmed/17228884?dopt=AbstractPlus]
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=628 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=625 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=626 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=627
Systematic nomenclatureNR3C4NR3C1NR3C2NR3C3
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:644, http://www.uniprot.org/uniprot/P10275 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7978, http://www.uniprot.org/uniprot/P04150 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:7979, http://www.uniprot.org/uniprot/P08235 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:8910, http://www.uniprot.org/uniprot/P06401
Rank order of potency http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2856 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2858 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2868, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2869 ≫ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2872, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3450 [http://www.ncbi.nlm.nih.gov/pubmed/8282004?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2869, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2868, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2872, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2377 [http://www.ncbi.nlm.nih.gov/pubmed/8282004?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2377
Endogenous agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2856 [http://www.ncbi.nlm.nih.gov/pubmed/2911578?dopt=AbstractPlus]– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2872 [http://www.ncbi.nlm.nih.gov/pubmed/10611474?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/8282004?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2377 [http://www.ncbi.nlm.nih.gov/pubmed/9667968?dopt=AbstractPlus]
Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7100 [http://www.ncbi.nlm.nih.gov/pubmed/17574413?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2859 [http://www.ncbi.nlm.nih.gov/pubmed/10852459?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2861 [http://www.ncbi.nlm.nih.gov/pubmed/17439112?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2857 [http://www.ncbi.nlm.nih.gov/pubmed/10076535?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6947 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7080 [http://www.ncbi.nlm.nih.gov/pubmed/10633034?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7076 [2], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7059 [2], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7088 [2], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7061 [2], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7434 [http://www.ncbi.nlm.nih.gov/pubmed/21880489?dopt=AbstractPlus]– http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2879 (Affinity at human PR‐A) [http://www.ncbi.nlm.nih.gov/pubmed/9464360?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3453, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2881 [http://www.ncbi.nlm.nih.gov/pubmed/6645495?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/14670641?dopt=AbstractPlus]
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2863 (pK i 7.7) [http://www.ncbi.nlm.nih.gov/pubmed/16420057?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6698 (pIC50 7.1–7.5) [http://www.ncbi.nlm.nih.gov/pubmed/18921992?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6812 (pIC50 7.4) [http://www.ncbi.nlm.nih.gov/pubmed/19359544?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2864 (pIC50 7.1–7.1) [http://www.ncbi.nlm.nih.gov/pubmed/9111629?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2862 (pEC50 6.6) [http://www.ncbi.nlm.nih.gov/pubmed/10076535?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8638 (pIC50 6.4) [http://www.ncbi.nlm.nih.gov/pubmed/15828836?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6943 (Displacement of 3[H] testosterone from wild‐type androgen receptors) (pK i 5.4) [http://www.ncbi.nlm.nih.gov/pubmed/18571420?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2882 (pIC50 7.6) [http://www.ncbi.nlm.nih.gov/pubmed/12781198?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3448 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8678 (pIC50 7.7) [http://www.ncbi.nlm.nih.gov/pubmed/22791416?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2876 (pK i 6.9) [http://www.ncbi.nlm.nih.gov/pubmed/18038968?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2882 (pIC50 6.3) [http://www.ncbi.nlm.nih.gov/pubmed/12781198?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3451, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3448 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7460 (pIC50 9.7) [http://www.ncbi.nlm.nih.gov/pubmed/18243712?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2805 (Mixed) (pK i 9) [http://www.ncbi.nlm.nih.gov/pubmed/12781197?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2882 (pK i 7.7) [http://www.ncbi.nlm.nih.gov/pubmed/8627601?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3448
Labelled ligands http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3455 (Selective Agonist), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3457 (Selective Agonist), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3456 (Agonist) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3447 (Agonist) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3452 (Selective Agonist) [http://www.ncbi.nlm.nih.gov/pubmed/16188378?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/6320679?dopt=AbstractPlus] – Rat http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3454 (Selective Agonist)
  55 in total

1.  Artesunate interacts with the vitamin D receptor to reverse sepsis-induced immunosuppression in a mouse model via enhancing autophagy.

Authors:  Shenglan Shang; Jiaqi Wu; Xiaoli Li; Xin Liu; Pan Li; Chunli Zheng; Yonghua Wang; Songqing Liu; Jiang Zheng; Hong Zhou
Journal:  Br J Pharmacol       Date:  2020-07-06       Impact factor: 8.739

2.  Inhibition of heparanase protects against pancreatic beta cell death in streptozotocin-induced diabetic mice via reducing intra-islet inflammatory cell infiltration.

Authors:  Wen-Yu Song; Xiao-Han Jiang; Ying Ding; Yan Wang; Ming-Xuan Zhou; Yun Xia; Chen-Yu Zhang; Chong-Chong Yin; Chen Qiu; Kai Li; Peng Sun; Xiao Han
Journal:  Br J Pharmacol       Date:  2020-08-19       Impact factor: 8.739

Review 3.  Immunoregulatory effects and therapeutic potential of vitamin D in multiple sclerosis.

Authors:  Wei Zhen Yeh; Melissa Gresle; Vilija Jokubaitis; Jim Stankovich; Anneke van der Walt; Helmut Butzkueven
Journal:  Br J Pharmacol       Date:  2020-08-05       Impact factor: 8.739

Review 4.  Old dog, new trick: Trivalent arsenic as an immunomodulatory drug.

Authors:  Yishan Ye; Béatrice Gaugler; Mohamad Mohty; Florent Malard
Journal:  Br J Pharmacol       Date:  2020-03-12       Impact factor: 8.739

5.  P2X7 receptor-targeted regulation by tetrahydroxystilbene glucoside in alcoholic hepatosteatosis: A new strategy towards macrophage-hepatocyte crosstalk.

Authors:  Yu Zhang; Min Jiang; Ben-Wen Cui; Cheng Hua Jin; Yan-Ling Wu; Yue Shang; Hong-Xu Yang; Mei Wu; Jian Liu; Chun-Ying Qiao; Zi-Ying Zhan; Huan Ye; Guang-Hao Zheng; Quan Jin; Li-Hua Lian; Ji-Xing Nan
Journal:  Br J Pharmacol       Date:  2020-02-23       Impact factor: 8.739

Review 6.  Function and therapeutic potential of G protein-coupled receptors in epididymis.

Authors:  Daolai Zhang; Yanfei Wang; Hui Lin; Yujing Sun; Mingwei Wang; Yingli Jia; Xiao Yu; Hui Jiang; Wenming Xu; Jin-Peng Sun; Zhigang Xu
Journal:  Br J Pharmacol       Date:  2020-10-29       Impact factor: 8.739

Review 7.  Protein phase separation: A novel therapy for cancer?

Authors:  Wei Wang; Yingqian Chen; Aixiao Xu; Minyi Cai; Ji Cao; Hong Zhu; Bo Yang; Xuejing Shao; Meidan Ying; Qiaojun He
Journal:  Br J Pharmacol       Date:  2020-09-28       Impact factor: 8.739

8.  Astaxanthin attenuates hepatic damage and mitochondrial dysfunction in non-alcoholic fatty liver disease by up-regulating the FGF21/PGC-1α pathway.

Authors:  Liwei Wu; Wenhui Mo; Jiao Feng; Jingjing Li; Qiang Yu; Sainan Li; Jie Zhang; Kan Chen; Jie Ji; Weiqi Dai; Jianye Wu; Xuanfu Xu; Yuqing Mao; Chuanyong Guo
Journal:  Br J Pharmacol       Date:  2020-06-27       Impact factor: 8.739

9.  A time-dependent contribution of hippocampal CB1 , CB2 and PPARγ receptors to cannabidiol-induced disruption of fear memory consolidation.

Authors:  Ana Maria Raymundi; Thiago R da Silva; Aleksander R Zampronio; Francisco S Guimarães; Leandro J Bertoglio; Cristina A J Stern
Journal:  Br J Pharmacol       Date:  2020-01-21       Impact factor: 8.739

10.  nNOS-CAPON blockers produce anxiolytic effects by promoting synaptogenesis in chronic stress-induced animal models of anxiety.

Authors:  Li-Juan Zhu; Hu-Jiang Shi; Lei Chang; Cheng Cheng Zhang; Meng Si; Na Li; Dong-Ya Zhu
Journal:  Br J Pharmacol       Date:  2020-05-28       Impact factor: 8.739
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.