| Literature DB >> 23754276 |
Ralf Brunner1, Caroline L Ng, Hamed Aissaoui, Myles H Akabas, Christoph Boss, Reto Brun, Paul S Callaghan, Olivier Corminboeuf, David A Fidock, Ithiel J Frame, Bibia Heidmann, Amélie Le Bihan, Paul Jenö, Corinna Mattheis, Suzette Moes, Ingrid B Müller, Michelle Paguio, Paul D Roepe, Romain Siegrist, Till Voss, Richard W D Welford, Sergio Wittlin, Christoph Binkert.
Abstract
A representative of a new class of potent antimalarials with an unknown mode of action was recently described. To identify the molecular target of this class of antimalarials, we employed a photo-reactive affinity capture method to find parasite proteins specifically interacting with the capture compound in living parasitized cells. The capture reagent retained the antimalarial properties of the parent molecule (ACT-213615) and accumulated within parasites. We identified several proteins interacting with the capture compound and established a functional interaction between ACT-213615 and PfMDR1. We surmise that PfMDR1 may play a role in the antimalarial activity of the piperazine-containing compound ACT-213615.Entities:
Keywords: ACT-213615; Affinity Capture; Drug Action; Mode of Action; Multidrug Transporters; PfMDR1; Photoaffinity Labeling; Plasmodium; Protein Drug Interactions
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Year: 2013 PMID： 23754276 PMCID： PMC3829344 DOI： 10.1074/jbc.M113.453159
Source DB: PubMed Journal: J Biol Chem ISSN： 0021-9258 Impact factor: 5.157