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 (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.15542. Enzymes are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors 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.

Highlights

  • Stephen PH Alexander1, Doriano Fabbro2, Eamonn Kelly3, Neil Marrion3, John A Peters4, Helen E Benson5, Elena Faccenda5, Adam J Pawson5, Joanna L Sharman5, Christopher Southan5, Jamie A Davies5 and CGTP Collaborators

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Summary

C13: Legumain C14: Caspase CE

Cysteine (C) Peptidases C48: Ulp endopeptidase M-: Metallo (M) Peptidases M79: Prenyl protease 2 MA: Metallo (M) Peptidases M1: Aminopeptidase N M2: Angiotensin-converting (ACE and ACE2) M10: Matrix metallopeptidase M12: Astacin/Adamalysin M13: Neprilysin M49: Dipeptidyl-peptidase III MC: Metallo (M) Peptidases M14: Carboxypeptidase A ME: Metallo (M) Peptidases M16: Pitrilysin MF: Metallo (M) Peptidases M17: Leucyl aminopeptidase MG: Metallo (M) Peptidases M24: Methionyl aminopeptidase MH: Metallo (M) Peptidases M18: Aminopeptidase I M20: Carnosine dipeptidase M28: Aminopeptidase Y MJ: Metallo (M) Peptidases M19: Membrane dipeptidase. T1: Proteasome T2: Glycosylasparaginase precursor PC: Cysteine (C) Peptidases C26: Gamma-glutamyl hydrolase SB: Serine (S) Peptidases. Serine palmitoyltransferase 3-ketodihydrosphingosine reductase Ceramide synthase Sphingolipid 1⁄24-desaturase Sphingomyelin synthase Sphingomyelin phosphodiesterase Neutral sphingomyelinase coupling factors Ceramide glucosyltransferase. 3.6.1.3 ATPases 2.1.1.- Protein arginine N-methyltransferases 3.5.1.- Histone deacetylases (HDACs) Cyclic nucleotide turnover Adenylyl cyclases Soluble guanylyl cyclase Exchange protein activated by cyclic AMP (Epac) Phosphodiesterases, 3’,5’-cyclic nucleotide. Haem oxygenase Hydrogen sulphide synthesis Hydrolases Inositol phosphate turnover Inositol 1,4,5-trisphosphate 3-kinases Inositol polyphosphate phosphatases Inositol monophosphatase Lanosterol biosynthesis pathway Nucleoside synthesis and metabolism. Thyroid hormone turnover 1.4.3.13 Lysyl oxidases 1.13.11.- Dioxygenases 1.14.11.29 2-oxoglutarate oxygenases transferases 2.3.-.- Acyltransferases 2.4.2.30 poly(ADP-ribose)polymerases 2.5.1.58 Protein farnesyltransferase 3.1.-.- Ester bond enzymes 3.1.1.- Carboxylic Ester Hydrolases 3.2.1.- Glycosidases 3.4.21.46 Complement factor D 3.5.1.- Histone deacetylases (HDACs) 3.5.3.15 Peptidyl arginine deiminases (PADI)

Small monomeric GTPases RAS subfamily
A22: Presenilin
C14: Caspase
1.14.13.30 Responsible for
2.5.1.58 Protein farnesyltransferase
Carbonate dehydratases
5.99.1.2 DNA Topoisomerases
5.99.1.2 DNA Topoisomerases 6105
Full Text
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