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 (http://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.

Highlights

  • 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

  • Overview: Retinoic acid receptors are nuclear hormone receptors of the NR1B family activated by the vitamin A-derived agonists tretinoin (ATRA) and alitretinoin, and the RAR-selective synthetic agonists TTNPB and adapalene

  • 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

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Summary

Citation for published version

Stephen PH and Cidlowski, John A and Kelly, Eamonn and Mathie, Alistair and Peters, John A and Veale, Emma L. and Armstrong, Jane F and Faccenda, Elena and Harding, Simon D and Pawson, Adam J and Sharman, Joanna L and Southan, Christopher and Davies, Jamie A and Coons, Laurel and Fuller, Peter and Korach, Kenneth S and Young, Morag (2019) THE CONCISE

Document Version
Family structure
Selective antagonists
Endogenous agonists Selective agonists
Selective antagonists Comments
Steroid hormone receptors
Endogenous agonists Selective agonists Selective antagonists
Full Text
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