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Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development
Authors:Chiranjeev Sharma  Myeong A Choi  Yoojin Song  Young Ho Seo
Affiliation:College of Pharmacy, Keimyung University, Daegu 704-701, Korea; (C.S.); (M.A.C.); (Y.S.)
Abstract:
PROTACs employ the proteosome-mediated proteolysis via E3 ligase and recruit the natural protein degradation machinery to selectively degrade the cancerous proteins. Herein, we have designed and synthesized heterobifunctional small molecules that consist of different linkers tethering KRIBB11, a HSF1 inhibitor, with pomalidomide, a commonly used E3 ligase ligand for anticancer drug development.
Keywords:HSF1   KRIBB11   PROTAC   thalidomide   anticancer drug development
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