Heterocyclic Compounds as CDK9 Inhibitors: Structural Diversity, Mechanism of Action, and Therapeutic Potential in Cancer and Beyond

被引：0
|
作者：
Bose, Kuntal [1 ]
Shajahan, Afiya [1 ]
Sreekumar, Nandana [1 ]
Aneesh, T. P. [1 ]
机构：
[1] Amrita Vishwa Vidyapeetham, Amrita Sch Pharm, Dept Pharmaceut Chem, AIMS Hlth Sci Campus, Kochi 682041, Kerala, India
来源：
CHEMISTRY & BIODIVERSITY | 2025年 / 22卷 / 01期
关键词：
CDK-9; P-TEFb; RNA polymerase-II; CTD; DEPENDENT KINASE INHIBITOR; CELL-CYCLE ARREST; R-ROSCOVITINE; PHASE-I; ANTITUMOR-ACTIVITY; TARGETING CDK9; DISCOVERY; FLAVOPIRIDOL; APOPTOSIS; COMBINATION;
D O I：
10.1002/cbdv.202401797
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Cyclin-dependent kinases (CDKs) are crucial proteins involved in key cellular processes, such as cell division and transcription. Their dysregulation plays a significant role in cancer development. Inhibiting cyclin-dependent kinase 9 (CDK9) impacts several survival pathways in cancer cells, presenting a promising therapeutic approach for various cancers. CDK9, in association with cyclin T1, forms the positive transcription elongation factor b (P-TEFb) complex, which phosphorylates the C-terminal domain (CTD) of RNA polymerase II (Pol II). This phosphorylation promotes the transition from transcription initiation to elongation. This review examines recent advancements in CDK9 modulators, with a particular emphasis on compounds currently in clinical trials.
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页数：16
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