Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D

被引:56
作者
Carroll, CD [1 ]
Johnson, TO
Tao, S
Lauri, G
Orlowski, M
Gluzman, IY
Goldberg, DE
Dolle, RE
机构
[1] Pharmacopeia Inc, Dept Biol, Princeton, NJ 08543 USA
[2] Pharmacopeia Inc, Dept Chem, Princeton, NJ 08543 USA
[3] Washington Univ, Howard Hughes Med Inst, Dept Med, St Louis, MO 63110 USA
[4] Washington Univ, Dept Mol Microbiol, St Louis, MO 63110 USA
关键词
D O I
10.1016/S0960-894X(98)00554-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P-1', P-2-P-4 surrogates. Evaluation of this encoded library against two aspartyl proteases, plasmepsin II and cathepsin D, led to the identification of selective inhibitors for each enzyme. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3203 / 3206
页数:4
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