Carroll C D, Johnson T O, Tao S, Lauri G, Orlowski M, Gluzman I Y, Goldberg D E, Dolle R E
Department of Biology, Pharmacopeia, Inc., Princeton, NJ 08543, USA.
Bioorg Med Chem Lett. 1998 Nov 17;8(22):3203-6. doi: 10.1016/s0960-894x(98)00554-x.
A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P1, P2-P4 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.
合成了一个基于结构的包含18900个成员的组合文库，其中含有一个他汀模板和三种环二氨基酸作为潜在的P1、P2 - P4替代物。用该编码文库对两种天冬氨酸蛋白酶（胃蛋白酶II和组织蛋白酶D）进行评估，从而鉴定出了针对每种酶的选择性抑制剂。
