鉴定新型UDP-葡萄糖4'-表异构酶抑制剂，该酶是非洲昏睡病的一个已验证的药物靶点。
Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness.
作者信息
Urbaniak Michael D, Tabudravu Jioji N, Msaki Aichi, Matera Kathy Mansfield, Brenk Ruth, Jaspars Marcel, Ferguson Michael A J
机构信息
Division of Biological Chemistry and Molecular Microbiology, School of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, UK.
出版信息
Bioorg Med Chem Lett. 2006 Nov 15;16(22):5744-7. doi: 10.1016/j.bmcl.2006.08.091. Epub 2006 Sep 7.
Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T. brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells.
通过筛选一个天然产物和市售类药物分子的小型文库，鉴定出了布氏锥虫和哺乳动物UDP - 葡萄糖4'-表异构酶的新型抑制剂。这些抑制剂在体外对布氏锥虫和人类酶具有低微摩尔效力，在两种酶之间表现出一定程度的选择性，并且对培养的布氏锥虫和哺乳动物细胞具有细胞毒性。
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