Target intelligence / Profile preview

Cyclin-dependent kinase 9 (CDK9)

Target
CDK9
Molecular classification
Serine/threonine protein kinase, Cyclin-dependent kinase (CDK), Enzyme
01

Overview

Cyclin-dependent kinase 9 (CDK9) is a serine/threonine kinase that plays a crucial role in transcriptional elongation by RNA polymerase II. It forms heterodimers with cyclins T1 or T2 to create Positive Transcription Elongation Factor b (P-TEFb), which phosphorylates the C-terminal domain of RNA polymerase II, promoting mRNA synthesis. CDK9 is also involved in recovery from replication stress and maintaining genome integrity. Dysregulation of CDK9 is linked to various cancers, making it an attractive therapeutic target.

02

Mechanism of action

Inhibition of CDK9 leads to downregulation of oncogenic drivers like c-MYC and induction of apoptosis in cancer cells.

03

Biological functions

Transcription regulationCell cycle controlStress responseMaintenance of genome integrity
04

Disease associations

CancerCardiac hypertrophy
05

Safety considerations

Potential side effect profiles compared to pan-CDK inhibitors.
06

Interacting drugs

Flavopiridol

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