Targeting the Hsp90 C-terminal domain to induce allosteric inhibition and selective client downregulation

Volume: 1861, Issue: 8, Pages: 1992 - 2006
Published: Aug 1, 2017
Abstract
Inhibition of Hsp90 is desirable due to potential downregulation of oncogenic clients. Early generation inhibitors bind to the N-terminal domain (NTD) but C-terminal domain (CTD) inhibitors are a promising class because they do not induce a heat shock response. Here we present a new structural class of CTD binding molecules with a unique allosteric inhibition mechanism.A hit molecule, NSC145366, and structurally similar probes were assessed for...
Paper Details
Title
Targeting the Hsp90 C-terminal domain to induce allosteric inhibition and selective client downregulation
Published Date
Aug 1, 2017
Volume
1861
Issue
8
Pages
1992 - 2006
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