Fluorescent inhibitors for IspF, an enzyme in the non-mevalonate pathway for isoprenoid biosynthesis and a potential target for antimalarial therapy

被引：37
|
作者：
Crane, CM
Kaiser, J
Ramsden, NL
Lauw, S
Rohdich, F
Eisenreich, W
Hunter, WN
Bacher, A
Diederich, F
机构：
[1] Univ Dundee, Sch Life Sci, Div Biol Chem & Mol Microbiol, Dundee DD1 5EH, Scotland
[2] Tech Univ Munich, Lehrstuhl Organ Chem & Biochem, D-85748 Garching, Germany
[3] ETH Honggerberg, Organ Chem Lab, CH-8093 Zurich, Switzerland
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2006年 / 45卷 / 07期
关键词：
fluorescence; inhibitors; IspF; non-mevalonate pathway; protein crystal structure analysis;
D O I：
10.1002/anie.200503003
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Designed inhibitors (like 1) of IspF, a key enzyme in the non-mevalonate pathway for terpene biosynthesis and a potential antimalarial target, were synthesized and evaluated. Since fluorescent probes were introduced in these ligands, their affinity towards IspF from E. coli could be determined by fluorescence titrations. The binding modes of two ligands in ternary complexes with IspF and a ZnII ion were clarified by X-ray analysis. (Chemical Equation Presented). © 2006 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码：1069 / 1074
页数：6
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