期刊
CHEMICAL COMMUNICATIONS
卷 53, 期 54, 页码 7577-7580出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c7cc03879h
关键词
-
资金
- NIH [CA182820, CA197999, CA054807, CA009476, CA036727]
- UNMC fellowship
- GAANN fellowship
Cyclin-dependent kinase 9 (CDK9), a member of the cyclindependent protein kinase (CDK) family, is involved in transcriptional elongation of several target genes. CDK9 is ubiquitously expressed and has been shown to contribute to a variety of malignancies such as pancreatic, prostate and breast cancers. Here we report the development of a heterobifunctional small molecule proteolysis targeting chimera (PROTAC) capable of cereblon (CRBN) mediated proteasomal degradation of CDK9. In HCT116 cells, it selectively degrades CDK9 while sparing other CDK family members. This is the first example of a PROTAC that selectively degrades CDK9.
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