Novel alpha-glucosidase inhibitors identified using multiple cyclic peptide combinatorial libraries

被引:28
作者
Eichler, J
Lucka, AW
Pinilla, C
Houghten, RA
机构
[1] Torrey Pines Institute for Molecular Studies, San Diego, CA 92121
关键词
synthetic combinatorial libraries; cyclic peptide libraries; alpha-glucosidase inhibitors;
D O I
10.1007/BF01715527
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Twenty-six cyclic synthetic peptide combinatorial libraries (disulfides and lactams) of varying size and composition, representing 6.8 x 10(3) to 4.7 x 10(7) individual peptides, were synthesized along with their respective linear analogs. One of the hexapeptide lactam libraries (cyclo[xXxXxN]) was found to have significant alpha-glucosidase inhibitory activity. This library was carried through an iterative process of synthesis and screening, during which all of the five mixture positions (x and X) were successively defined. As the result of this process, potent and selective alpha-glucosidase inhibitors were identified.
引用
收藏
页码:233 / 240
页数:8
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