| Literature DB >> 24528237 |
Stephen P H Alexander1, Helen E Benson, Elena Faccenda, Adam J Pawson, Joanna L Sharman, John C McGrath, William A Catterall, Michael Spedding, John A Peters, Anthony J Harmar, N Abul-Hasn, C M Anderson, C M H Anderson, M S Araiksinen, M Arita, E Arthofer, E L Barker, C Barratt, N M Barnes, R Bathgate, P M Beart, D Belelli, A J Bennett, N J M Birdsall, D Boison, T I Bonner, L Brailsford, S Bröer, P Brown, G Calo, W G Carter, W A Catterall, S L F Chan, M V Chao, N Chiang, A Christopoulos, J J Chun, J Cidlowski, D E Clapham, S Cockcroft, M A Connor, H M Cox, A Cuthbert, F M Dautzenberg, A P Davenport, P A Dawson, G Dent, J P Dijksterhuis, C T Dollery, A C Dolphin, M Donowitz, M L Dubocovich, L Eiden, K Eidne, B A Evans, D Fabbro, C Fahlke, R Farndale, G A Fitzgerald, T M Fong, C J Fowler, J R Fry, C D Funk, A H Futerman, V Ganapathy, B Gaisnier, M A Gershengorn, A Goldin, I D Goldman, A L Gundlach, B Hagenbuch, T G Hales, J R Hammond, M Hamon, J C Hancox, R L Hauger, D L Hay, A J Hobbs, M D Hollenberg, N D Holliday, D Hoyer, N A Hynes, K-I Inui, S Ishii, K A Jacobson, G E Jarvis, M F Jarvis, R Jensen, C E Jones, R L Jones, K Kaibuchi, Y Kanai, C Kennedy, I D Kerr, A A Khan, M J Klienz, J P Kukkonen, J Y Lapoint, R Leurs, E Lingueglia, J Lippiat, S J Lolait, S C R Lummis, J W Lynch, D MacEwan, J J Maguire, I L Marshall, J M May, C A McArdle, J C McGrath, M C Michel, N S Millar, L J Miller, V Mitolo, P N Monk, P K Moore, A J Moorhouse, B Mouillac, P M Murphy, R R Neubig, J Neumaier, B Niesler, A Obaidat, S Offermanns, E Ohlstein, M A Panaro, S Parsons, R G Pwrtwee, J Petersen, J-P Pin, D R Poyner, S Prigent, E R Prossnitz, N J Pyne, S Pyne, J G Quigley, R Ramachandran, E L Richelson, R E Roberts, R Roskoski, R A Ross, M Roth, G Rudnick, R M Ryan, S I Said, L Schild, G J Sanger, K Scholich, A Schousboe, G Schulte, S Schulz, C N Serhan, P M Sexton, D R Sibley, J M Siegel, G Singh, R Sitsapesan, T G Smart, D M Smith, T Soga, A Stahl, G Stewart, L A Stoddart, R J Summers, B Thorens, D T Thwaites, L Toll, J R Traynor, T B Usdin, R J Vandenberg, C Villalon, M Vore, S A Waldman, D T Ward, G B Willars, S J Wonnacott, E Wright, R D Ye, A Yonezawa, M Zimmermann.
Abstract
The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of the key properties of over 2000 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties from the IUPHAR database. The full contents can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/full. This compilation of the major pharmacological targets is divided into seven areas of focus: G protein-coupled receptors, ligand-gated ion channels, ion channels, catalytic receptors, nuclear hormone receptors, transporters and enzymes. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. A new landscape format has easy to use tables comparing related targets. It is a condensed version of material contemporary to late 2013, which is presented in greater detail and constantly updated on the website www.guidetopharmacology.org, superseding data presented in previous Guides to Receptors & Channels. It is produced in conjunction with NC-IUPHAR and provides the official IUPHAR classification and nomenclature for human drug targets, where appropriate. It consolidates information previously curated and displayed separately in IUPHAR-DB and GRAC and provides a permanent, citable, point-in-time record that will survive database updates.Entities:
Mesh:
Substances:
Year: 2013 PMID: 24528237 PMCID: PMC3892286 DOI: 10.1111/bph.12444
Source DB: PubMed Journal: Br J Pharmacol ISSN: 0007-1188 Impact factor: 8.739
| Nomenclature | Adipo1 receptor | Adipo2 receptor |
| HGNC, UniProt | ADIPOR1, Q96A54 | ADIPOR2, Q86V24 |
| Rank order of potency | globular adiponectin > adiponectin | globular adiponectin adiponectin |
| Preferred abbreviation | FABP1 | FABP2 | FABP3 | FABP4 | FABP5 |
| Nomenclature | fatty acid binding protein 1, liver | fatty acid binding protein 2, intestinal | fatty acid binding protein 3, muscle and heart (mammary-derived growth inhibitor) | fatty acid binding protein 4, adipocyte | fatty acid binding protein 5 (psoriasis-associated) |
| HGNC, UniProt | FABP1, P07148 | FABP2, P12104 | FABP3, P05413 | FABP4, P15090 | FABP5, Q01469 |
| Rank order of potency | stearic acid, oleic acid > palmitic acid, linoleic acid > arachidonic acid, α-linolenic acid | stearic acid > palmitic acid, oleic acid > linoleic acid > arachidonic acid, α-linolenic acid | stearic acid, oleic acid, palmitic acid > linoleic acid, α-linolenic acid, arachidonic acid | oleic acid, palmitic acid, stearic acid, linoleic acid > α-linolenic acid, arachidonic acid | – |
| Comment | A broader substrate specificity than other FABPs, binding two fatty acids per protein | Crystal structure of the rat FABP2 | Crystal structure of the human FABP3 | – | Crystal structure of the human FABP5 |
| Preferred abbreviation | FABP6 | FABP7 | FABP8 | FABP9 | FABP12 |
| Nomenclature | fatty acid binding protein 6, ileal | fatty acid binding protein 7, brain | peripheral myelin protein 2 | fatty acid binding protein 9, testis | fatty acid binding protein 12 |
| HGNC, UniProt | FABP6, P51161 | FABP7, O15540 | PMP2, P02689 | FABP9, Q0Z7S8 | FABP12, A6NFH5 |
| Comment | Able to transport bile acids | Crystal structure of the human FABP7 | – | – |
| Preferred abbreviation | RBP1 | RBP2 | RBP3 | RBP4 | RBP5 |
| Nomenclature | retinol binding protein 1, cellular | retinol binding protein 2, cellular | retinol binding protein 3, interstitial | retinol binding protein 4, plasma | retinol binding protein 5, cellular |
| HGNC, UniProt | RBP1, P09455 | RBP2, P50120 | RBP3, P10745 | RBP4, P02753 | RBP5, P82980 |
| Rank order of potency | – | stearic acid > palmitic acid, oleic acid, linoleic acid, α-linolenic acid, arachidonic acid | – | – | – |
| Preferred abbreviation | RBP7 | RLBP1 | CRABP1 | CRABP2 |
| Nomenclature | retinol binding protein 7, cellular | retinaldehyde binding protein 1 | cellular retinoic acid binding protein 1 | cellular retinoic acid binding protein 2 |
| HGNC, UniProt | RBP7, Q96R05 | RLBP1, P12271 | CRABP1, P29762 | CRABP2, P29373 |
| Rank order of potency | – | 11-cis-retinal, 11-cis-retinol > 9-cis-retinal, 13-cis-retinal, 13-cis-retinol, all-trans-retinal, retinol | all-trans-retinoic acid > 9-cis-retinoic acid stearic acid > palmitic acid, oleic acid, linoleic acid, α-linolenic acid, arachidonic acid | – |
| Nomenclature | σ1 (sigma non-opioid intracellular receptor 1) | σ2 |
| HGNC, UniProt | SIGMAR1, Q99720 | – |
| Selective agonists | (+)-SK&F10047, (RS)-PPCC (p | PB-28 (p |
| Selective antagonists | NE-100 (pIC50 8.4) | (RS)-SM21 (pIC50 7.2) |
| Radioligands ( | [3H]-pentazocine (Agonist) | [3H]-di-o-tolylguanidine (Agonist) |