TY - JOUR
T1 - Is PfCRT a channel or a carrier? Two competing models explaining chloroquine resistance in Plasmodium falciparum
AU - Sanchez, Cecilia P.
AU - Stein, Wilfred D.
AU - Lanzer, Michael
PY - 2007/7
Y1 - 2007/7
N2 - Chloroquine (CQ), an antimalarial drug with a long history, now frequently fails in the field owing to the rapid spread of resistant Plasmodium falciparum strains. CQ resistance is linked to a K76T mutation in PfCRT, a membrane-located food vacuolar protein and member of the drug-metabolite transporter superfamily, but there is as yet no agreed mechanism of how mutated PfCRT brings about CQ resistance. Current models suggest that mutated PfCRT acts either as a channel or a transporter of CQ, enabling CQ to leave the digestive food vacuole of the parasite, in which the CQ accumulates. Here, we review the pros and cons of the carrier and transporter models in light of recent developments in the field.
AB - Chloroquine (CQ), an antimalarial drug with a long history, now frequently fails in the field owing to the rapid spread of resistant Plasmodium falciparum strains. CQ resistance is linked to a K76T mutation in PfCRT, a membrane-located food vacuolar protein and member of the drug-metabolite transporter superfamily, but there is as yet no agreed mechanism of how mutated PfCRT brings about CQ resistance. Current models suggest that mutated PfCRT acts either as a channel or a transporter of CQ, enabling CQ to leave the digestive food vacuole of the parasite, in which the CQ accumulates. Here, we review the pros and cons of the carrier and transporter models in light of recent developments in the field.
UR - http://www.scopus.com/inward/record.url?scp=34250644012&partnerID=8YFLogxK
U2 - 10.1016/j.pt.2007.04.013
DO - 10.1016/j.pt.2007.04.013
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C2 - 17493873
AN - SCOPUS:34250644012
SN - 1471-4922
VL - 23
SP - 332
EP - 339
JO - Trends in Parasitology
JF - Trends in Parasitology
IS - 7
ER -
