TY - JOUR
T1 - Efflux of chloroquine from Plasmodium falciparum
T2 - Mechanism of chloroquine resistance
AU - Krogstad, Donald J.
AU - Gluzman, Ilya Y.
AU - Kyle, Dennis E.
AU - Oduola, Ayoade M.J.
AU - Martin, Samuel K.
AU - Milhous, Wilbur K.
AU - Schlesinger, Paul H.
PY - 1987/1/1
Y1 - 1987/1/1
N2 - Chloroquine-resistant Plasmodium falciparum accumulate significantly less chloroquine than susceptible parasites, and this is thought to be the basis of their resistance. However, the reason for the lower accumulation of chloroquine was unknown. The resistant parasite has now been found to release chloroquine 40 to 50 times more rapidly than the susceptible parasite, although their initial rates of chloroquine accumulation are the same. Verapamil and two other calcium channel blockers, as well as vinblastine and daunomycin, each slowed the release and increased the accumulation of chloroquine by resistant (but not susceptible) Plasmodium falciparum. These results suggest that a higher rate of chloroquine release explains the lower chloroquine accumulation, and thus the resistance observed in resistant Plamodium falciparum.
AB - Chloroquine-resistant Plasmodium falciparum accumulate significantly less chloroquine than susceptible parasites, and this is thought to be the basis of their resistance. However, the reason for the lower accumulation of chloroquine was unknown. The resistant parasite has now been found to release chloroquine 40 to 50 times more rapidly than the susceptible parasite, although their initial rates of chloroquine accumulation are the same. Verapamil and two other calcium channel blockers, as well as vinblastine and daunomycin, each slowed the release and increased the accumulation of chloroquine by resistant (but not susceptible) Plasmodium falciparum. These results suggest that a higher rate of chloroquine release explains the lower chloroquine accumulation, and thus the resistance observed in resistant Plamodium falciparum.
UR - http://www.scopus.com/inward/record.url?scp=0023666563&partnerID=8YFLogxK
U2 - 10.1126/science.3317830
DO - 10.1126/science.3317830
M3 - Article
C2 - 3317830
AN - SCOPUS:0023666563
VL - 238
SP - 1283
EP - 1285
JO - Science
JF - Science
SN - 0036-8075
IS - 4831
ER -