CDK9 inhibitors in cancer research
Zhi Huang1,2, Tianqi Wang1, Cheng Wang1
1Department of Medicinal Chemistry, School of Medicine, Nankai University 94 Weijin Road Tianjin 300071 China yanfan@nankai.edu.cn.
Abstract:
Cyclin dependent kinase 9 (CDK9) plays an essential role in regulating transcriptional elongation. Aberrations in CDK9 activity have been observed in various cancers, which make CDK9 an attractive therapeutic target for cancers. This led to an intensive development of small-molecule CDK9 inhibitors or new emerging strategies, such as proteolysis targeting chimeras (PROTACs). Here, we review the CDK9 modulators in cancer not only for research purposes, but also for therapeutic applications.
Insights
Cyclin-dependent kinase 9 (CDK9) is crucial for gene transcription and a target in cancer therapy. This review covers CDK9 inhibitors and PROTACs for cancer research and treatment.
Area of Science:
- Molecular Biology
- Cancer Biology
- Drug Discovery
Background:
- Cyclin-dependent kinase 9 (CDK9) is vital for transcriptional elongation.
- Altered CDK9 activity is implicated in various cancers, presenting it as a therapeutic target.
Purpose of the Study:
- To review CDK9 modulators for cancer research.
- To discuss therapeutic applications of CDK9 inhibitors and PROTACs.
Main Methods:
- Literature review of CDK9 modulators.
- Analysis of small-molecule inhibitors and PROTACs targeting CDK9.
Main Results:
- CDK9 is a validated target in oncology.
- Development of small-molecule inhibitors and PROTACs shows promise.
Conclusions:
- CDK9 modulators offer significant potential for cancer therapy.
- Further research into CDK9-targeted strategies is warranted.
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