Kinases (EC 2.7.x.x)

Overview

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Protein serine/threonine kinases (E.C. 2.7.11.-) use the co-substrate ATP to phosphorylate serine and/or threonine residues on target proteins. Analysis of the human genome suggests the presence of 518 protein kinases in man, with over 100 protein kinase-like pseudogenes [2]. It is beyond the scope of the Guide to list all these protein kinase activities; this summary focuses on AGC protein kinases associated with GPCR signalling, which may be divided into 15 subfamilies in man.

Most inhibitors of these enzymes have been assessed in cell-free investigations and so may appear to ‘lose’ potency and selectivity in intact cell assays. In particular, ambient ATP concentrations may be influential in responses to inhibitors, since the majority are directed at the ATP binding site [1] .

Subfamilies

Further reading

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Kinases (EC 2.7.x.x). Accessed on 18/12/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=698.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: Enzymes. Br J Pharmacol. 170: 1797–1867.