Beierle John M, Horne W Seth, van Maarseveen Jan H, Waser Beatrice, Reubi Jean Claude, Ghadiri M Reza
Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Angew Chem Int Ed Engl. 2009;48(26):4725-9. doi: 10.1002/anie.200805901.
A would-be amide: A 1,4-disubstituted 1,2,3-triazole was used as a surrogate for a trans amide bond to create a library of 16 diastereomeric pseudotetrapeptides as beta-turn mimetics. High-resolution structural analysis indicated that these scaffolds adopt distinct, rigid, conformationally homogeneous beta-turn-like structures (see example), some of which bind somatostatin receptor subtypes selectively, and some of which show broad-spectrum activity.
使用1,4-二取代的1,2,3-三唑作为反式酰胺键的替代物,构建了一个包含16种非对映异构假四肽的文库作为β-转角模拟物。高分辨率结构分析表明,这些支架采用独特、刚性、构象均一的β-转角样结构(见示例),其中一些选择性结合生长抑素受体亚型,一些表现出广谱活性。