Detection, Characterization, and Screening of Heme-Binding Molecules by Mass Spectrometry for Malaria Drug Discovery

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• 作者：Katalina Mu帽oz-Durango ; Alexandre Maciuk ; Abha Harfouche ; Sandra Torijano-Guti茅rrez ; Jean-Christophe Jullian ; J茅r么me Quintin ; Kevin Spelman ; Elisabeth Mouray ; Philippe Grellier ; Bruno Figad猫re
• 刊名：Analytical Chemistry
• 出版年：2012
• 出版时间：April 3, 2012
• 年：2012
• 卷：84
• 期：7
• 页码：3324-3329
• 全文大小：278K
• 年卷期：v.84,no.7(April 3, 2012)
• ISSN：1520-6882

文摘

Drug screening for antimalarials uses heme biocrystallization inhibition methods as an alternative to parasite cultures, but they involve complex processes and cannot detect artemisinin-like molecules. The described method detects heme-binding compounds by mass spectrometry, using dissociation of the drug鈥揾eme adducts to evaluate putative antiplasmodial activity. Applied to a chemical library, it showed a good hit-to-lead ratio and is an efficient early stage screening for complex mixtures like natural extracts.