title: Detection, characterization, and screening of heme-binding molecules by mass spectrometry for malaria drug discovery.
abstract: 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-heme 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.
authors.affiliation: Laboratoire de Pharmacognosie, UMR 8076 CNRS BioCIS, Faculté de Pharmacie, Université Paris-Sud, 5 rue J.-B. Clément, 92296 Châtenay-Malabry, France.
authors.forename: Katalina
authors.initials: K
authors.lastname: Muñoz-Durango
authors.forename: Alexandre
authors.initials: A
authors.lastname: Maciuk
authors.forename: Abha
authors.initials: A
authors.lastname: Harfouche
authors.forename: Sandra
authors.initials: S
authors.lastname: Torijano-Gutiérrez
authors.forename: Jean-Christophe
authors.initials: JC
authors.lastname: Jullian
authors.forename: Jérôme
authors.initials: J
authors.lastname: Quintin
authors.forename: Kevin
authors.initials: K
authors.lastname: Spelman
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Mouray
authors.forename: Philippe
authors.initials: P
authors.lastname: Grellier
authors.forename: Bruno
authors.initials: B
authors.lastname: Figadère
mesh_terms: D000962:Antimalarials / Q000032:analysis* / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology; D055808:Drug Discovery / Q000379:methods*; D006418:Heme / Q000737:chemistry*; D013058:Mass Spectrometry / Q000379:methods*
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D006418:Heme; C031327:artemisinin