On the mechanism of chloroquine resistance in Plasmodium falciparum.

ABSTRACT: Resistance to chloroquine of malaria strains is known to be associated with a parasite protein named PfCRT, the mutated form of which is able to reduce chloroquine accumulation in the digestive vacuole of the pathogen. Whether the protein mediates extrusion of the drug acting as a channel or as a carrier and which is the protonation state of its chloroquine substrate is the subject of a scientific debate. We present here an analytical approach that explores which combination of hypotheses on the mechanism of transport and the protonation state of chloroquine are consistent with available equilibrium experimental data. We show that the available experimental data are not, by themselves, sufficient to conclude whether the protein acts as a channel or as a transporter, which explains the orig

SUBMITTER: Chinappi M 

PROVIDER: S-EPMC2988812 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature