Drug Discovery for Neglected Diseases: Molecular Target-Based and Phenotypic Approaches

被引：160

作者：

Gilbert, Ian H. ^{[1
]}

机构：

[1] Univ Dundee, Coll Life Sci, Div Biol Chem & Drug Discovery, Drug Discovery Unit, Dundee DD1 5EH, Scotland

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 56卷 / 20期

基金：

英国惠康基金;

关键词：

PROTEIN N-MYRISTOYLTRANSFERASE; PTERIDINE REDUCTASE 1; CANDIDA-ALBICANS; MYRISTOYL-COA; PEPTIDOMIMETIC INHIBITORS; TRYPANOSOMA-BRUCEI; DIHYDROOROTATE DEHYDROGENASE; SELECTIVE INHIBITORS; CROSS-RESISTANCE; DIPEPTIDE AMIDES;

D O I：

10.1021/jm400362b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Drug discovery for neglected tropical diseases is carried out using both target-based and phenotypic approaches. In this paper, target-based approaches are discussed, with a particular focus on human African trypanosomiasis. Target-based drug discovery can be successful, but careful selection of targets is required. There are still very few fully validated drug targets in neglected diseases, and there is a high attrition rate in target-based drug discovery for these diseases. Phenotypic screening is a powerful method in both neglected and non-neglected diseases and has been very successfully used. Identification of molecular targets from phenotypic approaches can be a way to identify potential new drug targets.

引用

页码：7719 / 7726

页数：8

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