期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 19, 页码 5041-5049出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.02.063
关键词
Plk1; Selectivity; Polo-box domain; Cryptic binding pocket
资金
- Center for Cancer Research, National Cancer Institute, National Institutes of Health, United States
- NATIONAL CANCER INSTITUTE [ZIABC006198] Funding Source: NIH RePORTER
An important goal in the development of polo-like kinase 1 (Plk1) polo-box domain (PBD) binding inhibitors is selectivity for Plk1 relative to Plk2 and Plk3. In our current work we show that Plk1 PBD selectivity can be significantly enhanced by modulating interactions within a previously discovered cryptic pocket and a more recently identified proximal auxiliary pocket. Published by Elsevier Ltd.
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