Cyclin-dependent kinase (CDK) family C

Overview

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Five of the cyclin-dependent kinases (CDKs: 7, 8, 9, 12, and 13) are involved in the phosphorylation of serine residues in the C-terminal domain of RNA polymerase II, the enzyme that is responsible for the transcription of protein-coding genes into mRNA in eukaryotes. Phosphorylation of RNA polymerase II at Ser5 is essential for transcriptional initiation, and phosphorylation of Ser 2 contributes to transcriptional elongation and termination. All five of the C-terminal domain kinases can phosphorylate Ser5, but only CDK9, CDK12, and CDK13 can phosphorylate at Ser2 [1-3].

Subfamilies

GtoImmuPdb view: ON    Families that contain targets of relevance to immunopharmacology are highlighted in blue

The Kinome image shown here was obtained from Chartier et al. (2013, <a href='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3740139/figure/fig-4/' target='_blank'>Figure 4</a>) <a href='https://www.ncbi.nlm.nih.gov/pubmed/23940838' target='_blank'>https://www.ncbi.nlm.nih.gov/pubmed/23940838</a> and has been annotated to show the kinases that are targeted by currently approved kinase inhibitor drugs (last updated in April 2018).

Comments

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The development of CDK inhibitors as anticancer drugs is reviewed in [4], with detailed content covering CDK4 and CDK6 inhibitors that are under clinical evaluation.

References

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How to cite this family page

Database page citation:

Cyclin-dependent kinase (CDK) family. Accessed on 10/12/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=453.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2017) The Concise Guide to PHARMACOLOGY 2017/18: Enzymes. Br J Pharmacol. 174 Suppl 1: S272-S359.