INTERACTION OF A PEPTIDOMIMETIC AMINIMIDE INHIBITOR WITH ELASTASE

被引：44

作者：

PEISACH, E

CASEBIER, D

GALLION, SL

FURTH, P

PETSKO, GA

HOGAN, JC

RINGE, D

机构：

[1] BRANDEIS UNIV, DEPT BIOCHEM, WALTHAM, MA 02254 USA

[2] BRANDEIS UNIV, DEPT CHEM, WALTHAM, MA 02254 USA

[3] BRANDEIS UNIV, ROSENSTIEL BASIC MED SCI RES CTR, WALTHAM, MA 02254 USA

[4] BRANDEIS UNIV, PROGRAM BIOPHYS, WALTHAM, MA 02254 USA

来源：

SCIENCE | 1995年 / 269卷 / 5220期

关键词：

D O I：

10.1126/science.7604279

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

The crystal structure of an aminimide analog of a dipeptide inhibitor of porcine pancreatic elastase bound to its target serine protease has been solved. The peptidomimetic molecule binds in the same fashion as the class of dipeptides from which it was derived, making similar interactions with the subsites on the elastase surface. Because aminimides are readily synthesized from a wide variety of starting materials, they form the basis for a combinatorial chemistry approach to rational drug design.

引用

页码：66 / 69

页数：4

共 23 条

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