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.

中文翻译：

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封面文章：作为Hsp90 C末端抑制剂的Stilbene类似物的合成和生物学评估（ChemMedChem 24/2017）

掩盖特征揭示了带有客体蛋白底物的动画复合物中的热激蛋白90（Hsp90），客体蛋白底物代表了治疗上寻求的致癌靶标。当具有适当大小和形状的抑制剂结合Hsp90时，蛋白质折叠机制将被破坏，客户蛋白质将被降解。这项工作集中于阐明最近公开的基于的Hsp90抑制剂的构效关系。具有三唑酰胺侧链，叔胺，总长度约为24Å的化合物表现出由Hsp90抑制引起的低纳摩尔抗增殖活性。可以在Brian S. J. Blagg等人的论文全文中找到更多信息。就在第24期，2017年2022页。