Mechanism-based inactivation of E-coli gamma-glutamylcysteine synthetase by phosphinic acid- and sulfoximine-based transition-state analogues

被引：26

作者：

Katoh, M ^{[1
]}

Hiratake, J ^{[1
]}

Kato, H ^{[1
]}

Oda, J ^{[1
]}

机构：

[1] KYOTO UNIV,INST CHEM RES,UJI,KYOTO 611,JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(96)00247-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Phosphinic acid- and sulfoximine-based transition state analogues having a carboxyl group at the beta-carbon to the hetero atom exhibited significantly higher potency as mechanism-based inhibitors of E. coli gamma-glutamylcysteine synthetase as compared with L-buthionine-SR-sulfoximine. The enhanced inhibition potency is evidenced by both tight binding of the inhibitor and slow enzyme reactivation. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1437 / 1442

页数：6

共 15 条

[1]

Brolin S. E, 1983, METHOD ENZYMAT AN, V3, P540

[2] ANALYTICAL AND PREPARATIVE SEPARATION OF THE DIASTEREOMERS OF L-BUTHIONINE (SR)-SULFOXIMINE, A POTENT INHIBITOR OF GLUTATHIONE BIOSYNTHESIS [J].