Bilayer effects of antimalarial compounds Academic Article uri icon

Overview

MeSH Major

  • Antimalarials
  • Lipid Bilayers

abstract

  • Because of the perpetual development of resistance to current therapies for malaria, the Medicines for Malaria Venture developed the Malaria Box to facilitate the drug development process. We tested the 80 most potent compounds from the box for bilayer-mediated effects on membrane protein conformational changes (a measure of likely toxicity) in a gramicidin-based stopped flow fluorescence assay. Among the Malaria Box compounds tested, four compounds altered membrane properties (p< 0.05); MMV007384 stood out as a potent bilayer-perturbing compound that is toxic in many cell-based assays, suggesting that testing for membrane perturbation could help identify toxic compounds. In any case, MMV007384 should be approached with caution, if at all.

publication date

  • November 9, 2015

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC4638347

Digital Object Identifier (DOI)

  • 10.1371/journal.pone.0142401

PubMed ID

  • 26551613

Additional Document Info

start page

  • e0142401

volume

  • 10

number

  • 11