抗疟药物的全球表型筛选。
Global phenotypic screening for antimalarials.
作者信息
Guiguemde W Armand, Shelat Anang A, Garcia-Bustos Jose F, Diagana Thierry T, Gamo Francisco-Javier, Guy R Kiplin
机构信息
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA.
出版信息
Chem Biol. 2012 Jan 27;19(1):116-29. doi: 10.1016/j.chembiol.2012.01.004.
Abstract
Malaria, a devastating infectious disease caused by Plasmodium spp., leads to roughly 655,000 deaths per year, mostly of African children. To compound the problem, drug resistance has emerged to all classical antimalarials and may be emerging for artemisinin-based combination therapies. To address the need for new antimalarials with novel mechanisms, several groups carried out phenotypic screening campaigns to identify compounds inhibiting growth of the blood stages of Plasmodium falciparum. In this review, we describe the characterization of these compounds, explore currently ongoing strategies to develop lead molecules, and endorse the concept of a "malaria box" of publicly accessible active compounds.
摘要
疟疾是由疟原虫属引起的一种毁灭性传染病，每年导致约65.5万人死亡，其中大多数是非洲儿童。更糟糕的是，所有传统抗疟药物都出现了耐药性，基于青蒿素的联合疗法也可能出现耐药性。为满足对具有新作用机制的新型抗疟药物的需求，多个研究小组开展了表型筛选活动，以鉴定抑制恶性疟原虫血液阶段生长的化合物。在本综述中，我们描述了这些化合物的特性，探讨了目前正在进行的开发先导分子的策略，并支持建立一个可公开获取的活性化合物“疟疾盒”的概念。
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