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

CDK12 (Q9NYV4) - Overview - Molecular Target Synopsis

Protein


CDK12, Cyclin-dependent kinase 12
Enzyme Classification 2.7.11.22
UniProt Q9NYV4

Also Known as CDK12_HUMAN, CDK12, CRK7, CRKRS, KIAA0904

Cyclin-dependent kinase that phosphorylates the C-terminal domain (CTD) of the large subunit of RNA polymerase II (POLR2A), thereby acting as a key regulator of transcription elongation. Regulates the expression of genes involved in DNA repair and is required for the maintenance of genomic stability. Preferentially phosphorylates 'Ser-5' in CTD repeats that are already phosphorylated at 'Ser-7', but can also phosphorylate 'Ser-2'. Required for RNA splicing, possibly by phosphorylating SRSF1/SF2. Involved in regulation of MAP kinase activity, possibly leading to affect the response to estrogen inhibitors. Interacts with CCNL1 and CCNL2 (By similarity). Interacts with CCNK.

6CKX
STRUCTURE OF CDK12/CYCK IN COMPLEX WITH A SMALL MOLECULE INHIBITOR N- (4-(1-METHYL-1H-PYRAZOL-4-YL)PHENYL)-N-((1R,4R)-4-(QUINAZOLIN-2- YLAMINO)CYCLOHEXYL)ACETAMIDE
RCSB/PDB
Inspect Structure
See all 3D Structures for CDK12

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project CDK12 has gain in 18 cell-lines, loss in 3 cell-lines and no signal in 984 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-N87, JIMT-1, MKN-7

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


For CDK12 there are:
6 structures (12 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CDK12 has been screened with compounds ( bioactivities). (see details)