CDK1 subfamily

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Targets
Enzymes
Kinases (EC 2.7.x.x)
CMGC: Containing CDK, MAPK, GSK3, CLK families
Cyclin-dependent kinase (CDK) family
CDK1 subfamily

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Enzymes

CDK1 (cyclin dependent kinase 1) Show summary »« Hide summary More detailed page go icon to follow link

CDK2 (cyclin dependent kinase 2) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1973

Nomenclature

cyclin dependent kinase 2

Common abbreviation

CDK2

Previous and unofficial names

cell division protein kinase 2

Genes

CDK2 (Hs), Cdk2 (Mm), Cdk2 (Rn)

Ensembl ID

ENSG00000123374 (Hs), ENSMUSG00000025358 (Mm), ENSRNOG00000006469 (Rn)

UniProtKB AC

P24941 (Hs), P97377 (Mm), Q63699 (Rn)

EC number

2.7.11.22

Inhibitors

R547 pK_d 9.3 [4]

BMS-387032 pK_d 7.2 [4]

R547 pK_i 8.5 [5]

dinaciclib pIC₅₀ 9.0 [11]

compound 9b [PMID: 18986805] pIC₅₀ >9.0 [8]

BS-194 pIC₅₀ 8.5 [6]

compound 3 [PMID: 19097791] pIC₅₀ 8.4 [14]

milciclib pIC₅₀ 7.3 [1]

AT-7519 pIC₅₀ 7.3 [12]

alvocidib pIC₅₀ 6.4 – 7.0 [2,10]

Selective inhibitors

BMS-265246 pIC₅₀ 8.1 [13]

Comment

CDK2 drives G1/S cell cyle progression. Its inhibition produces an anti-tumour effect that is mediated by induction of cell cycle arrest and apoptosis (which inhibits tumour cell proliferation) and by enhancing antitumour immunity (via activation of the type I IFN response and increasing tumour antigen presentation) [3].

CDK3 (cyclin dependent kinase 3) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1975

Nomenclature

cyclin dependent kinase 3

Common abbreviation

CDK3

Previous and unofficial names

Cdkn3 | Cell division protein kinase 3 | cyclin-dependent kinase 3 | cyclin-dependent kinase 3, pseudogene | Cdk3-ps

Genes

CDK3 (Hs), Cdk3 (Mm)

Ensembl ID

ENSG00000250506 (Hs), ENSMUSG00000092300 (Mm)

UniProtKB AC

Q00526 (Hs), Q80YP0 (Mm)

EC number

2.7.11.22

References

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1. Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R et al.. (2009) Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem, 52 (16): 5152-63. [PMID:19603809]

2. Carlson BA, Dubay MM, Sausville EA, Brizuela L, Worland PJ. (1996) Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (CDK) 2 and CDK4 in human breast carcinoma cells. Cancer Res, 56 (13): 2973-8. [PMID:8674031]

3. Chen Y, Cai Q, Pan C, Liu W, Li L, Liu J, Gao M, Li X, Wang L, Rao Y et al.. (2022) CDK2 Inhibition Enhances Antitumor Immunity by Increasing IFN Response to Endogenous Retroviruses. Cancer Immunol Res, 10 (4): 525-539. [PMID:35181784]

4. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

5. DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R et al.. (2006) In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol Cancer Ther, 5 (11): 2644-58. [PMID:17121911]

6. Heathcote DA, Patel H, Kroll SH, Hazel P, Periyasamy M, Alikian M, Kanneganti SK, Jogalekar AS, Scheiper B, Barbazanges M et al.. (2010) A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem, 53 (24): 8508-22. [PMID:21080703]

7. Jiang X, Zhao B, Britton R, Lim LY, Leong D, Sanghera JS, Zhou BB, Piers E, Andersen RJ, Roberge M. (2004) Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide. Mol Cancer Ther, 3 (10): 1221-7. [PMID:15486189]

8. Jones CD, Andrews DM, Barker AJ, Blades K, Byth KF, Finlay MR, Geh C, Green CP, Johannsen M, Walker M et al.. (2008) Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett, 18 (24): 6486-9. [PMID:18986805]

9. Joshi KS, Rathos MJ, Joshi RD, Sivakumar M, Mascarenhas M, Kamble S, Lal B, Sharma S. (2007) In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. Mol Cancer Ther, 6 (3): 918-25. [PMID:17363486]

10. Losiewicz MD, Carlson BA, Kaur G, Sausville EA, Worland PJ. (1994) Potent inhibition of CDC2 kinase activity by the flavonoid L86-8275. Biochem Biophys Res Commun, 201 (2): 589-95. [PMID:8002990]

11. Martin MP, Olesen SH, Georg GI, Schönbrunn E. (2013) Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chem Biol, 8 (11): 2360-5. [PMID:24007471]

12. Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, Lyons JF, Thompson NT. (2009) Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther, 8 (2): 324-32. [PMID:19174555]

13. Sutherland JJ, Low J, Blosser W, Dowless M, Engler TA, Stancato LF. (2011) A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther, 10 (2): 242-54. [PMID:21216932]

14. Trujillo JI, Kiefer JR, Huang W, Thorarensen A, Xing L, Caspers NL, Day JE, Mathis KJ, Kretzmer KK, Reitz BA et al.. (2009) 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor. Bioorg Med Chem Lett, 19 (3): 908-11. [PMID:19097791]

How to cite this family page

Database page citation:

CDK1 subfamily. Accessed on 08/12/2023. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=492.

Concise Guide to PHARMACOLOGY citation:

Alexander SP, Fabbro D, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Enzymes. Br J Pharmacol. 178 Suppl 1:S313-S411.