Rapid Development of a Potent Photo-triggered Inhibitor of the Serine Hydrolase RBBP9

被引：11

作者：

Liu, Xiaodan ^{[3
]}

Dix, Melissa ^{[1
,2
]}

Speers, Anna E. ^{[1
,2
]}

Bachovchin, Daniel A. ^{[1
,2
]}

Zuhl, Andrea M. ^{[1
,2
]}

Cravatt, Benjamin F. ^{[1
,2
]}

Kodadek, Thomas J. ^{[3
]}

机构：

[1] Scripps Res Inst, Dept Chem Physiol, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA

[3] Scripps Res Inst, Dept Chem, Jupiter, FL 33458 USA

来源：

CHEMBIOCHEM | 2012年 / 13卷 / 14期

关键词：

ABPP; CALI; one-bead-one-compound; peptoid librarys; RBBP9; serine hydrolases; ASSISTED LASER INACTIVATION; CYCLIC PEPTIDYL INHIBITORS; COMBINATORIAL LIBRARIES; CROSS-LINKING; PROTEINS; IDENTIFICATION; SYSTEM; LIGHT; BEAD;

D O I：

10.1002/cbic.201200445

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：

The serine hydrolases constitute a large class of enzymes that play important roles in physiology. There is great interest in the development of potent and selective pharmacological inhibitors of these proteins. Traditional active-site inhibitors often have limited selectivity within this superfamily and are tedious and expensive to discover. Using the serine hydrolase RBBP9 as a model target, we designed a rapid and relatively inexpensive route to highly selective peptoid-based inhibitors that can be activated by visible light. This technology provides rapid access to photo-activated tool compounds capable of selectively blocking the function of particular serine hydrolases.

引用

页码：2082 / 2093

页数：12

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