Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay

被引：40
|
作者：
Dubowchik, GM [1 ]
Ditta, JL [1 ]
Herbst, JJ [1 ]
Bollini, S [1 ]
Vinitsky, A [1 ]
机构：
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 06期
关键词：
D O I：
10.1016/S0960-894X(00)00045-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Several fluoresceinated FKBP12 ligands have been prepared for a high-throughput fluorescence polarization assay. K(i)s for FKBP12 rotamase inhibition by these ligands range from 1.3 mu M to 32 nM, and their design is based on X-ray crystal structures of FKBP12 complexed with known immunophilin ligands. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：559 / 562
页数：4
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