Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Targeting the thyroid-stimulating hormone receptor with small molecule ligands and antibodies.

Literature DB >> 25768836

Targeting the thyroid-stimulating hormone receptor with small molecule ligands and antibodies.

Abstract

INTRODUCTION: The thyroid-stimulating hormone receptor (TSHR) is the essential molecule for thyroid growth and thyroid hormone production. Since it is also a key autoantigen in Graves' disease and is involved in thyroid cancer pathophysiology, the targeting of the TSHR offers a logical model for disease control. AREAS COVERED: We review the structure and function of the TSHR and the progress in both small molecule ligands and TSHR antibodies for their therapeutic potential. EXPERT OPINION: Stabilization of a preferential conformation for the TSHR by allosteric ligands and TSHR antibodies with selective modulation of the signaling pathways is now possible. These tools may be the next generation of therapeutics for controlling the pathophysiological consequences mediated by the effects of the TSHR in the thyroid and other extrathyroidal tissues.

Entities: CellLine Chemical Disease Gene Species

Keywords: Graves’ disease; autoantibodies; glycoprotein-hormone receptor; small molecule ligands; thyroid cancer; thyroid-stimulating hormone receptor

Mesh：

Substances：

Year: 2015 PMID： 25768836 PMCID： PMC4484771 DOI： 10.1517/14728222.2015.1018181

Source DB: PubMed Journal: Expert Opin Ther Targets ISSN： 1472-8222 Impact factor: 6.902

94 in total

1. Severe embryopathy and exposure to methimazole in early pregnancy.

Authors: F Anders Karlsson; Ove Axelsson; Håkan Melhus
Journal: J Clin Endocrinol Metab Date: 2002-02 Impact factor: 5.958

2. Crystal structure of the TSH receptor (TSHR) bound to a blocking-type TSHR autoantibody.

Authors: Paul Sanders; Stuart Young; Jane Sanders; Katarzyna Kabelis; Stuart Baker; Andrew Sullivan; Michele Evans; Jill Clark; Jane Wilmot; Xiaoling Hu; Emma Roberts; Michael Powell; Ricardo Núñez Miguel; Jadwiga Furmaniak; Bernard Rees Smith
Journal: J Mol Endocrinol Date: 2011-02-15 Impact factor: 5.098

3. Role of amino acids 261-418 in proteolytic cleavage of the extracellular region of the human thyrotropin receptor.

Authors: D Russo; Y Nagayama; G D Chazenbalk; H L Wadsworth; B Rapoport
Journal: Endocrinology Date: 1992-04 Impact factor: 4.736

4. Gbetagamma dimers released in response to thyrotropin activate phosphoinositide 3-kinase and regulate gene expression in thyroid cells.

Authors: Miguel A Zaballos; Bibian Garcia; Pilar Santisteban
Journal: Mol Endocrinol Date: 2008-01-17

5. Heterogeneous responses of recombinant human thyrotropin receptor to immunoglobulins from patients with Graves' disease.

Authors: T Endo; M Ohmori; M Ikeda; E Anzai; T Onaya
Journal: Biochem Biophys Res Commun Date: 1992-08-14 Impact factor: 3.575

6. Graves' IgG recognizes linear epitopes in the human thyrotropin receptor.

Authors: E V Nagy; H B Burch; K Mahoney; Y G Lukes; J C Morris; K D Burman
Journal: Biochem Biophys Res Commun Date: 1992-10-15 Impact factor: 3.575

7. A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR).

Authors: Holger Jäschke; Susanne Neumann; Susanna Moore; Craig J Thomas; Anny-Odile Colson; Stefano Costanzi; Gunnar Kleinau; Jian-Kang Jiang; Ralf Paschke; Bruce M Raaka; Gerd Krause; Marvin C Gershengorn
Journal: J Biol Chem Date: 2006-02-16 Impact factor: 5.157

8. Folding of the recombinant human thyrotropin (TSH) receptor extracellular domain: identification of folded monomeric and tetrameric complexes that bind TSH receptor autoantibodies.

Authors: P N Graves; H Vlase; T F Davies
Journal: Endocrinology Date: 1995-02 Impact factor: 4.736

9. A stimulatory TSH receptor antibody enhances adipogenesis via phosphoinositide 3-kinase activation in orbital preadipocytes from patients with Graves' ophthalmopathy.

Authors: Seema Kumar; Sarah Nadeem; Marius N Stan; Michael Coenen; Rebecca S Bahn
Journal: J Mol Endocrinol Date: 2011-04-12 Impact factor: 5.098

10. Advances in graves' disease.

Authors: Juan C Galofré; Leonidas H Duntas; L D Premawardhana; Terry F Davies
Journal: J Thyroid Res Date: 2012-05-20

13 in total

Review 1. The cell biology of the thyroid-disrupting mechanism of dichlorodiphenyltrichloroethane (DDT).

Authors: M Rossi; A R Taddei; I Fasciani; R Maggio; F Giorgi
Journal: J Endocrinol Invest Date: 2017-06-21 Impact factor: 4.256

2. Inhibiting thyrotropin/insulin-like growth factor 1 receptor crosstalk to treat Graves' ophthalmopathy: studies in orbital fibroblasts in vitro.

Authors: Robert F Place; Christine C Krieger; Susanne Neumann; Marvin C Gershengorn
Journal: Br J Pharmacol Date: 2017-01-27 Impact factor: 8.739

3. Modulating TSH Receptor Signaling for Therapeutic Benefit.

Authors: Gerd Krause; Anja Eckstein; Ralf Schülein
Journal: Eur Thyroid J Date: 2020-11-23

4. Critical Differences between Induced and Spontaneous Mouse Models of Graves' Disease with Implications for Antigen-Specific Immunotherapy in Humans.

Authors: Basil Rapoport; Bianca Banuelos; Holly A Aliesky; Nicole Hartwig Trier; Sandra M McLachlan
Journal: J Immunol Date: 2016-11-09 Impact factor: 5.422

Review 10. Bioassays for TSH Receptor Autoantibodies, from FRTL-5 Cells to TSH Receptor-LH/CG Receptor Chimeras: The Contribution of Leonard D. Kohn.

Authors: Cesidio Giuliani; Motoyasu Saji; Ines Bucci; Giorgio Napolitano
Journal: Front Endocrinol (Lausanne) Date: 2016-07-25 Impact factor: 5.555