Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

CDK3 (Q00526) - Overview - Molecular Target Synopsis

Protein


CDK3, Cyclin-dependent kinase 3
Enzyme Classification 2.7.11.22
UniProt Q00526

Also Known as CDK3_HUMAN, CDK3, CDKN3

Serine/threonine-protein kinase that plays a critical role in the control of the eukaryotic cell cycle; involved in G0-G1 and G1-S cell cycle transitions. Interacts with CCNC/cyclin-C during interphase. Phosphorylates histone H1, ATF1, RB1 and CABLES1. ATF1 phosphorylation triggers ATF1 transactivation and transcriptional activities, and promotes cell proliferation and transformation. CDK3/cyclin-C mediated RB1 phosphorylation is required for G0-G1 transition. Promotes G1-S transition probably by contributing to the activation of E2F1, E2F2 and E2F3 in a RB1-independent manner. Interacts with CABLES1 and CABLES2 (By similarity). Interacts with ATF1. Binding to CCNC/cyclin-C promotes RB1 phosphorylation.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
305ENSG00000250506ENST00000448471, ENST00000425876ENSP00000400088, ENSP00000410561Q00526-1

Sub-cellular localization


GO terms: CDK3 is active in the following subcellular-locations: nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CDK3 has gain in 7 cell-lines, loss in 0 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_5, COLO205, T47D

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H209, GTL-16

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, HSMM

(see details)

3D Structures


At greater than 75% identity similarity to CDK3 there are:
210 structures (250 chains) solved
195 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

CDK3 is solved in complex with the approved drug(s):

B49/SUNITINIB (3TI1_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CDK3 has been screened with 775 compounds (1405 bioactivities), 93 compounds have bioactivities that show binding affinity of <= 500nM (100 bioactivities). (see details)