THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors

Abstract

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 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 (https://www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes over 500 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/bph.15538. G protein‐coupled receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: ion channels, nuclear hormone 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‐2021, and supersedes data presented in the 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC‐IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

Long‐term antagonism and allosteric regulation of mu opioid receptors by the novel ligand, methocinnamox

“…Key protein targets and ligands in this article are hyperlinked to corresponding entries in http://www.guidetopharmacology.org , the common portal for data from the IUPHAR/BPS Guide to Pharmacology, 26 and are permanently archived in the Concise Guide to Pharmacology 2021/22. 27 …”

Adenosine Receptor Antagonists to Combat Cancer and to Boost Anti-Cancer Chemotherapy and Immunotherapy

“…Before the cloning technique was available, pharmacological tools allowed the discovery of 3 receptors that were named as A 1 , A 2 and A 3 ; one more receptor was identified by cloning its cDNA, and the nomenclature that holds today is: A 1 , A 2A , A 2B and A 3 . Whereas A 1 and A 3 receptors couple to G i/o , whose engagement leads to reduction in the activity of the adenylyl cyclase, the canonical proteins that couple to A 2A or to A 2B receptors are of the G s family, whose engagement leads to an increase in the activity of the adenylyl cyclase [ 2 ]. A comprehensive review on adenosine receptors and cancer was written in 2009 by Fishman et al [ 7 ].…”

“…Twenty years ago, it was discovered that oral administration of a muscle cell conditioned medium inhibited tumor growth in mice [ 1 ]. Adenosine was responsible for the effect and the action was mainly mediated by the A 3 receptor, which is one of the four identified proteins that sense extracellular adenosine: A 1 , A 2A , A 2B and A 3 [ 2 ] (see below for a general description of adenosine receptors). Interestingly, it was postulated that, in addition to adenosine, muscle cells produced other compounds (“stable, nondegradable”) that behave as agonists of the A 3 receptor (A 3 R) [ 1 ].…”

Membrane Melatonin Receptors Activated Cell Signaling in Physiology and Disease

“…Melatonin receptors were named for their endogenous ligand melatonin, which is abbreviated as “MT” using capital letters, and each type of receptor was denoted by a numerical subscript (i.e., MT1, MT2). According to the “Concise Guide to PHARMACOLOGY 2015/16” [ 21 ] produced in conjunction with NC-IUPHAR to provide the official IUPHAR classification and nomenclature for human drug targets, melatonin receptors are included in the rhodopsin family (Class A) of G protein-coupled receptors and are activated by the endogenous ligands melatonin and N-acetylserotonin, as well as by clinically used drugs like ramelteon, agomelatine and tasimelteon [ 22 ]. MT1/MT2 heterodimers present different pharmacological profiles from MT1 and MT2 receptors.…”