ACS Chem Biol. 2012 Apr 20;7(4):637-45. doi: 10.1021/cb2003175. Epub 2012 Jan 26.
A new synthetic strategy for obtaining artificial receptors that selectively regulate and/or control specific protein/protein interactions was developed based on the template-assisted and the self-activating click reaction applied to a combinatorial library. Synthetic mimics of the Grb2-SH2 domain, examined as a model case, selectively bound to a target signaling protein to induce cytotoxicity and inhibit tumor growth in vivo.
开发了一种新的合成策略,用于获得人工受体,这些受体可以选择性地调节和/或控制特定的蛋白质/蛋白质相互作用,该策略基于模板辅助和自激活点击反应应用于组合文库。作为模型案例研究的 Grb2-SH2 结构域的合成模拟物选择性地与靶信号蛋白结合,以在体内诱导细胞毒性并抑制肿瘤生长。