Volonterio Alessandro, Moisan Lionel, Rebek Julius
The Skaggs Institute for Chemical Biology and Department of Chemistry, The Scripps Research Institute MB-26, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
Org Lett. 2007 Sep 13;9(19):3733-6. doi: 10.1021/ol701487g. Epub 2007 Aug 21.
The synthesis of several amphiphilic, nonpeptidic scaffolds that mimic the presentation of i, i + 3 or i + 4, and i + 7 residues of a peptide alpha-helix is described. The approach uses a pyridazine core, and the synthesis involves only a few steps and minimizes the number of C-C bond-forming reactions. The versatility of the synthesis makes it suitable for the preparation of small libraries of low molecular weight alpha-helix mimetics that could be targeted to certain protein/protein interactions.
本文描述了几种两亲性非肽支架的合成方法,这些支架模拟了肽α-螺旋中i、i + 3或i + 4以及i + 7位残基的排列方式。该方法采用哒嗪核心,合成仅涉及几个步骤,并将碳-碳键形成反应的数量降至最低。合成的多功能性使其适用于制备可针对特定蛋白质/蛋白质相互作用的低分子量α-螺旋模拟物的小型文库。