Cover Feature: Synthesis and Biological Evaluation of Stilbene Analogues as Hsp90 C‐Terminal Inhibitors (ChemMedChem 24/2017)
Year: 2017
Type: article
Abstract: The Cover Feature reveals heat shock protein 90 (Hsp90) in an animated complex with client protein substrates that represent therapeutically sought after oncogenic targets. When an inhibitor of appropriate size and shape binds Hsp90, the protein folding machinery is disrupted and the client proteins degraded. This work focused on the elucidation of structure–activity relationships for the recently disclosed stilbene-based Hsp90 inhibitors. Compounds with a triazole-containing amide side chain, tertiary amine, and an overall length of ∼24 Å manifested low nanomolar antiproliferative activity that results from Hsp90 inhibition. More information can be found in the Full Paper by Brian S. J. Blagg et al. on page 2022 in Issue 24, 2017.
Source: ChemMedChem
Institution: University of Notre Dame
Language: English
Topic: Heat shock proteins research
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: bronze
OpenAlex ID: W2780285109