TY - JOUR
T1 - Molecular Insights on Selective and Specific Inhibitors of Cyclin Dependent Kinase 9 Enzyme (CDK9) for the Purpose of Cancer Therapy
AU - Karati, Dipanjan
AU - Mahadik, Kaka Saheb Ramoo
AU - Trivedi, Piyush
AU - Kumar, Dileep
N1 - Publisher Copyright:
© 2023 Bentham Science Publishers.
PY - 2023/2
Y1 - 2023/2
N2 - Cyclin Dependent Kinase 9 (CDK9), which controls transcriptional elongation, is a promising pharmacological target for a variety of cancerous cells, specifically those characterized by transcriptional dysregulation. CDK9 promotes the pause or release of RNA polymerase II, a rate-limiting stage in normal transcriptional regulation that is often disturbed in cancers. New indications suggest that selective CDK9 antagonism may be beneficial in the treatment of some cancers. CDK9 modulators (inhibitors and degraders) have gained a lot of attention recently, and many molecules are currently in clinical trials. In this review, the CDK9 antagonists under clinical and preclinical trials have been discussed, as well as the structure-activity relationship has been studied, which will help scientists generate more tar-get-specific drug molecules in the future with less toxicity.
AB - Cyclin Dependent Kinase 9 (CDK9), which controls transcriptional elongation, is a promising pharmacological target for a variety of cancerous cells, specifically those characterized by transcriptional dysregulation. CDK9 promotes the pause or release of RNA polymerase II, a rate-limiting stage in normal transcriptional regulation that is often disturbed in cancers. New indications suggest that selective CDK9 antagonism may be beneficial in the treatment of some cancers. CDK9 modulators (inhibitors and degraders) have gained a lot of attention recently, and many molecules are currently in clinical trials. In this review, the CDK9 antagonists under clinical and preclinical trials have been discussed, as well as the structure-activity relationship has been studied, which will help scientists generate more tar-get-specific drug molecules in the future with less toxicity.
UR - https://www.scopus.com/pages/publications/85138372719
UR - https://www.scopus.com/pages/publications/85138372719#tab=citedBy
U2 - 10.2174/1871520622666220615125826
DO - 10.2174/1871520622666220615125826
M3 - Review article
C2 - 35708082
AN - SCOPUS:85138372719
SN - 1871-5206
VL - 23
SP - 383
EP - 403
JO - Anti-Cancer Agents in Medicinal Chemistry
JF - Anti-Cancer Agents in Medicinal Chemistry
IS - 4
ER -