THE MODE OF ACTION AND THE MECHANISM OF RESISTANCE TO ANTIMALARIAL-DRUGS

被引:113
作者
FOOTE, SJ
COWMAN, AF
机构
[1] WHITEHEAD INST BIOMED RES, 9 CAMBRIDGE CTR, CAMBRIDGE, MA 01242 USA
[2] ROYAL MELBOURNE HOSP, WALTER & ELIZA HALL INST MED RES, PARKVILLE, VIC 3050, AUSTRALIA
关键词
MALARIA; DRUG RESISTANCE; CHLOROQUINE; ANTIFOLATE; SULFA DRUG;
D O I
10.1016/0001-706X(94)90061-2
中图分类号
R38 [医学寄生虫学]; Q [生物科学];
学科分类号
07 ; 0710 ; 09 ; 100103 ;
摘要
The mechanism of action of the antifolate and quinoline antinialarials has been investigated over the last few decades, and recent advances should aid the development of new drugs to combat the increasingly refractile parasite. The molecular description of resistance to the antifolates has been well characterised and is due to structural changes in the target enzymes, but the factors involved in the parasite's ability to circumvent the action of the quinoline antimalarials have yet to be fully elucidated. This review discusses the mode of action of these drugs and the means used by the parasite to defeat our therapeutic ingenuity.
引用
收藏
页码:157 / 171
页数:15
相关论文
共 95 条
[1]  
AIKAWA M, 1972, AM J PATHOL, V67, P277
[2]  
ARMSTRONG VL, 1974, TOXICOL APPL PHARM, V29, P90
[3]   SELECTION FOR HIGH-LEVEL CHLOROQUINE RESISTANCE RESULTS IN DEAMPLIFICATION OF THE PFMDR1 GENE AND INCREASED SENSITIVITY TO MEFLOQUINE IN PLASMODIUM-FALCIPARUM [J].
BARNES, DA ;
FOOTE, SJ ;
GALATIS, D ;
KEMP, DJ ;
COWMAN, AF .
EMBO JOURNAL, 1992, 11 (08) :3067-3075
[4]   REVERSAL OF CHLOROQUINE RESISTANCE WITH DESIPRAMINE IN ISOLATES OF PLASMODIUM-FALCIPARUM FROM CENTRAL AND WEST-AFRICA [J].
BASCO, LK ;
LEBRAS, J .
TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE, 1990, 84 (04) :479-481
[5]   PLASMODIUM-FALCIPARUM - INVITRO DRUG-INTERACTION BETWEEN CHLOROQUINE AND ENANTIOMERS OF AMLODIPINE [J].
BASCO, LK ;
LEBRAS, J .
EXPERIMENTAL PARASITOLOGY, 1991, 72 (03) :262-270
[7]   REVERSAL OF CHLOROQUINE RESISTANCE IN MALARIA PARASITE PLASMODIUM-FALCIPARUM BY DESIPRAMINE [J].
BITONTI, AJ ;
SJOERDSMA, A ;
MCCANN, PP ;
KYLE, DE ;
ODUOLA, AMJ ;
ROSSAN, RN ;
MILHOUS, WK ;
DAVIDSON, DE .
SCIENCE, 1988, 242 (4883) :1301-1303
[8]  
BOLIN JT, 1982, J BIOL CHEM, V257, P13650
[9]   MEFLOQUINE-RESISTANT MALARIA INDUCED BY INAPPROPRIATE QUININE REGIMENS [J].
BRASSEUR, P ;
KOUAMOUO, J ;
DRUILHE, P .
JOURNAL OF INFECTIOUS DISEASES, 1991, 164 (03) :625-626
[10]  
BRASSEUR P, 1992, AM J TROP MED HYG, V46, P1