从一个编码的他汀组合文库中鉴定恶性疟原虫天冬氨酸蛋白酶II的有效抑制剂。
Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.
作者信息
Carroll C D, Patel H, Johnson T O, Guo T, Orlowski M, He Z M, Cavallaro C L, Guo J, Oksman A, Gluzman I Y, Connelly J, Chelsky D, Goldberg D E, Dolle R E
机构信息
Department of Biology, Pharmacopeia, Inc., Princeton, NJ 08540, USA.
出版信息
Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20. doi: 10.1016/s0960-894x(98)00419-3.
PMID:9873534
Abstract
An encoded 13,020-member combinatorial library was synthesized containing a statine core. Evaluation of this library with plasmepsin II, an aspartyl protease required for hemoglobin metabolism in the malaria parasite, led to the identification of potent and selective inhibitors as well as novel structure-activity relationships.
摘要
合成了一个包含13020个成员的编码组合文库，其含有一个他汀核心。用疟原虫血红蛋白代谢所需的天冬氨酸蛋白酶——胃蛋白酶II对该文库进行评估，从而鉴定出了强效和选择性抑制剂以及新的构效关系。
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