协调复合物 SH2 结构域模拟物：一种破坏致癌蛋白-蛋白相互作用的替代方法。
Coordination complex SH2 domain proteomimetics: an alternative approach to disrupting oncogenic protein-protein interactions.
机构信息
Department of Chemistry, University of Toronto, Toronto, Canada.
出版信息
Chem Commun (Camb). 2010 Feb 14;46(6):892-4. doi: 10.1039/b919608k. Epub 2009 Dec 1.
Abstract
We report the first application of coordination complexes as functional proteomimetics of the Src homology 2 (SH2) phosphopeptide-binding domain. As a proof-of-concept, functionalized bis-dipicolylamine (BDPA) copper(ii) complexes are shown to disrupt oncogenic Stat3-Stat3 protein complexes and elicit promising anti-tumour activity.
摘要
我们首次将配位化合物应用于Src 同源 2 (SH2) 磷酸肽结合结构域的功能模拟蛋白。作为概念验证，功能化双二吡啶基胺 (BDPA) 铜(ii) 配合物被证明可破坏致癌 Stat3-Stat3 蛋白复合物，并表现出有前景的抗肿瘤活性。
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