蛋白酶体抑制剂的抗锥虫活性。
Antitrypanosomal activities of proteasome inhibitors.
作者信息
Nkemngu Njinkeng Joseph, Rosenkranz Vera, Wink Michael, Steverding Dietmar
机构信息
Abteilung Parasitologie, Hygiene-Institut. Institut für Pharmazeutische Biologie, Ruprecht-Karls-Universität, Heidelberg, Germany.
出版信息
Antimicrob Agents Chemother. 2002 Jun;46(6):2038-40. doi: 10.1128/AAC.46.6.2038-2040.2002.
Abstract
Seven peptidyl proteasome inhibitors were tested for in vitro activity against Trypanosoma brucei bloodstream forms. Two compounds showed activity in the low nanomolar range. In general, trypanosomes were more susceptible to the compounds than were human HL-60 cells. The data support the potential of proteasome inhibitors for rational antitrypanosomal drug development.
摘要
测试了七种肽基蛋白酶体抑制剂对布氏锥虫血流形式的体外活性。两种化合物在低纳摩尔范围内显示出活性。总体而言，锥虫比人类HL-60细胞对这些化合物更敏感。这些数据支持蛋白酶体抑制剂在合理开发抗锥虫药物方面的潜力。
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