CATH Classification

Domain Context

CATH Clusters

Superfamily Transferase(Phosphotransferase) domain 1
Functional Family cyclin-dependent kinase 12 isoform X1

Enzyme Information

2.7.11.23
[RNA-polymerase]-subunit kinase.
based on mapping to UniProt Q9NYV4
ATP + [DNA-directed RNA polymerase] = ADP + [DNA-directed RNA polymerase] phosphate.
-!- Appears to be distinct from other protein phosphokinases. -!- Brings about multiple phosphorylation of the unique C-terminal repeat domain of the largest subunit of eukaryotic EC 2.7.7.6. -!- Does not phosphorylate casein, phosvitin or histone. -!- Formerly EC 2.7.1.141.
2.7.11.22
Cyclin-dependent kinase.
based on mapping to UniProt Q9NYV4
ATP + a protein = ADP + a phosphoprotein.
-!- Activation of cyclin-dependent kinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. -!- It is the sequential activation and inactivation of cyclin-dependent kinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation. -!- Formerly EC 2.7.1.37.

UniProtKB Entries (1)

Q9NYV4
CDK12_HUMAN
Homo sapiens
Cyclin-dependent kinase 12

PDB Structure

PDB 6CKX
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.
Ito, M., Tanaka, T., Toita, A., Uchiyama, N., Kokubo, H., Morishita, N., Klein, M.G., Zou, H., Murakami, M., Kondo, M., Sameshima, T., Araki, S., Endo, S., Kawamoto, T., Morin, G.B., Aparicio, S.A., Nakanishi, A., Maezaki, H., Imaeda, Y.
J. Med. Chem.