期刊
PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS
卷 74, 期 1, 页码 122-132出版社
WILEY
DOI: 10.1002/prot.22136
关键词
cyclin dependent kinase; peptide inhibitor; binding pocket; cell cycle; computer docking simulations
资金
- Conrad
- George Washington University REF, SE
- NIH [AI065236, AI043894]
- NSF [DMR0313129]
- NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [R01AI043894, R21AI065236] Funding Source: NIH RePORTER
The cyclin-dependent kinase 2 (cdk2) is a serine/threonine protein kinase that plays a key role in the cell cycle control system of all eukaryotic organisms. It has been a much studied drug target for potential anticancer therapy. Most cdk2 inhibitors in clinical development target almost exclusively the catalytic ATP-binding pocket of cdk2. However, several five amino-acid peptide inhibitors that are directed towards a noncatalytic binding pocket of cdk2 are reported here. Upon binding to this new pocket located at the cdk2 and cyclin interface, these peptide inhibitors are found to disrupt the cdk2/cyclin E complex partially and diminish its kinase activity in vitro.
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