PTEF-b/CDK9 Inhibitor BAY1251152
An inhibitor of cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II (RNA Pol II) elongation factor positive transcription elongation factor b (PTEF- b; PTEFb), with potential antineoplastic activity. Upon administration, BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins. This may cause cell cycle arrest and induce apoptosis, which may lead to a reduction in tumor cell proliferation. The protein complex PTEF-b, a heterodimer consisting of CDK9 and a regulatory cyclin subunit of the T family, is over-activated in various tumor cell types; it plays a key role in the regulation of Pol II-mediated transcription of anti-apoptotic proteins. Tumor cells are dependent on anti-apoptotic proteins for their survival. [ ]
Term info
PTEF-b/CDK9 Inhibitor BAY1251152
- BAY 1251152
- BAY1251152
- CDK9 Inhibitor BAY1251152
- PTEF-b Inhibitor BAY1251152
- PTEF-b/CDK9 Inhibitor BAY1251152
NCIT_C116978, NCIT_C128784, NCIT_C157711, NCIT_C116977, NCIT_C157712
CTRP
PTEF-b/CDK9 Inhibitor BAY1251152
http://purl.obolibrary.org/obo/NCIT_C25842
CL507865
PTEF-b/CDK9 Inhibitor BAY1251152
Pharmacologic Substance
C128266
Term relations
- Cyclin-Dependent Kinase Inhibitor
- Chemical_Or_Drug_Has_Physiologic_Effect some Gene Regulation Process
- Chemical_Or_Drug_Has_Mechanism_Of_Action some Enzyme Inhibition
- Chemical_Or_Drug_Has_Physiologic_Effect some Positive Regulation of Apoptosis
- Chemical_Or_Drug_Has_Physiologic_Effect some Protein Phosphorylation Inhibition
- Chemical_Or_Drug_Affects_Gene_Product some Cyclin-Dependent Kinase