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• W4382400227 abstract "Despite the early clinical promise, adverse events such as acquired resistance and dose-limiting toxicities have barred the widespread use of HSP90 inhibitors as anticancer drugs. A new approach involving proteolysis-targeting chimeras (PROTACs) to degrade the protein instead of inhibiting it may overcome these problems. In this work, we describe the design, synthesis, and evaluation of cereblon-recruiting geldanamycin-based HSP90 degraders based on the PROTAC technology. Our best degrader, 3a , effectively decreased HSP90α and HSP90β levels in cells utilizing the ubiquitin–proteasome pathway." @default.
• W4382400227 created "2023-06-29" @default.
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• W4382400227 date "2023-06-28" @default.
• W4382400227 modified "2023-10-14" @default.
• W4382400227 title "Development of the first geldanamycin-based HSP90 degraders" @default.
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• W4382400227 doi "https://doi.org/10.3389/fchem.2023.1219883" @default.
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