Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay

被引：41

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

页码：559 / 562

页数：4

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