生物素化 sansalvamide A 类似物的合成与评价及其对 Hsp90 的调节作用。
Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90.
机构信息
Department of Chemistry and Biochemistry, 5500 Campanile Drive, San Diego State University, San Diego, CA 92182-1030, United States.
出版信息
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4716-9. doi: 10.1016/j.bmcl.2011.06.083. Epub 2011 Jun 25.
Abstract
Described are the syntheses of three sansalvamide A derivatives that contain biotinylated tags at individual positions around the macrocycle. The tagged derivatives indicated in protein pull-down assays that they bind to Hsp90 at the same binding site (N-Middle domain) as the San A-amide peptide. Further, these compounds inhibit binding between Hsp90 and multiple C-terminal client proteins. This interaction is unique to the San A analogs indicating they can be tuned for selectivity against Hsp90 client/co-chaperone proteins.
摘要
描述了三种含有生物素标记的 sansalvamide A 衍生物的合成，这些标记分别位于大环的各个位置。在蛋白下拉实验中，这些标记衍生物表明它们与 Hsp90 的结合位点（N-中端结构域）与 San A-酰胺肽相同。此外，这些化合物抑制了 Hsp90 与多个 C 端客户蛋白之间的结合。这种相互作用是 San A 类似物所特有的，表明它们可以针对 Hsp90 客户/共伴侣蛋白进行选择性调节。
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