Alternative mutations at position 76 of the vacuolar transmembrane protein PfCRT are associated with chloroquine resistance and unique stereospecific quinine and quinidine responses in Plasmodium falciparum

Molecular Pharmacology

Volumn 61, Issue 1, 2002, Pages 35-42

  Cooper, Roland A ^a   Ferdig, Michael T ^a   Su, Xin Zhuan ^a   Ursos, Lyann M B ^b   Mu, Jianbing ^a   Nomura, Takashi ^a,e   Fujioka, Hisashi ^c   Fidock, David A ^d   Roepe, Paul D ^b   Wellems, Thomas E ^a  

^a NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES   (United States)

^b GEORGETOWN UNIVERSITY   (United States)

^c CASE WESTERN RESERVE UNIVERSITY   (United States)

^d ALBERT EINSTEIN COLLEGE OF MEDICINE   (United States)

^e KYOTO UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CHLOROQUINE;

AMINO ACID SEQUENCE; ANTIMALARIAL ACTIVITY; ARTICLE; GENE MUTATION; MALARIA; NONHUMAN; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

ACRIDINE ORANGE; ANIMALS; ANTIMALARIALS; CALCIUM CHANNEL BLOCKERS; CHLOROQUINE; DRUG INTERACTIONS; DRUG RESISTANCE; FLUORESCENCE; MEMBRANE PROTEINS; MOLECULAR CONFORMATION; MUTATION; PARASITIC SENSITIVITY TESTS; PLASMODIUM FALCIPARUM; PROTOZOAN PROTEINS; QUINIDINE; QUININE; VERAPAMIL;

EID: 18244396971     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.61.1.35     Document Type: Article

References (45)

1. Plasmodium falciparum: Induction, selection, and characterization of pyrimethamine-resistant mutants
2. Selection for high-level chloroquine resistance results in deamplificatian of the pfmdr1 gene and increased sensitivity to mefloquine in Plasmodium falciparum
3. Uptake and efflux of chloroquine by chloroquine-resistant Plasmodium falciparum clones recently isolated in Africa
4. Relationship of global chloroquine transport and reversal of resistance in Plasmodium falciparum
5. Access to hematin: The basis of chloroquine resistance
6. Distribution of acridine orange fluorescence in Plasmodium falciparum-infected erythrocytes and its implications for the evaluation of digestive vacuole pH
7. Hemolysis of mouse erythrocytes by ferriprotoporphyrin IX and chloroquine. Chemotherapeutic implications
8. Plasmodium falciparum S-adenosylhomocysteine hydrolase. cDNA identification, predicted protein sequence, and expression in Escherichia coli
9. Aminoquinolines that circumvent resistance in Plasmodium falciparum in vitro
10. Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique
11. A molecular marker for chloroquine-resistant falciparum malaria
12. An assessment of drug-haematin binding as a mechanism for inhibition of haematin polymerisation by quinolone antimalarials
13. Susceptibility of African isolates of Plasmodium falciparum to artemisinin (qinghaosu)
14. Rates of spontaneous mutation
15. Digestive vacuolar pH of intact intraerythrocytic P. falciparum either sensitive or resistant to chloroquine
16. The transmembrane domain 10 of the yeast Pdr5p ABC antifungal efflux pump determines both substrate specificity and inhibitor susceptibility
17. Mutations in the P. falciparum digestive vacuole transmembrane protein PfCRT and evidence for their role in chloroquine resistance
18. Plasmodium falciparum in owl monkeys: Drug resistance and chloroquine binding capacity
19. Frequency of drug resistance in Plasmodium falciparum: A nonsynergistic combination of 5-fluoroorotate and atovaquone suppresses in vitro resistance
20. An integrated model of chloroquine action
21. A rapid in vitro test to chloroquine-resistant Plasmodium falciparum
22. Relationship between antimalarial drug activity, accumulation, and inhibition of heme polymerization in Plasmodium falciparum in vitro
23. The role of drug accumulation in 4-aminoquinoline antimalarial potency. The influence of structural substitution and physicochemical properties
24. Mutations in Plasmodium falciparum cytochrome b that are associated with atovaquone resistance are located at a putative drug-binding site
25. Energy dependence of chloroquine accumulation and chloroquine efflux in Plasmodium falciparum
26. Efflux of chloroquine from Plasmodium falciparum: Mechanism of chloroquine resistance
27. Synchronization of Plasmodium falciparum erythrocytic stages in culture
28. Plasmodium falciparum: Chloroquine selection of a cloned line and DNA rearrangements
29. Possible modes of action of the artemisinin-type compounds
30. Synthesis, antimalarial activity, and molecular modeling of tebuquine analogues
31. +/dicarboxylate co-transporter NaDC-1
32. Spread of chloroquine resistance in Plasmodium falciparum
33. Variations in frequencies of drug resistance in Plasmodium falciparum
34. Pgh1 modulates sensitivity and resistance to multiple antimalarials in Plasmodium falciparum
35. 4-Aminoquinoline analogs of chloroquine with shortened side chains retain activity against chloroquine-resistant Plasmodium falciparum
36. Identification of a chloroquine importer in Plasmodium falciparum. Differences in import kinetics are genetically linked with the chloroquine-resistant phenotype
37. Complex polymorphisms in an approximately 330 kDa protein are linked to chloroquine-resistant P. falciparum in Southeast Asia and Africa
38. Plasmodium falciparum: Parasite typing by using a multicopy microsatellite marker, PfRRM
39. Plasmodium falciparum: Assignment of microsatellite markers to chromosomes by PFG-PCR
40. A common mechanism for blockade of heme polymerization by antimalarial quinolines
41. Dihydrofolate reductase mutations and chromosomal changes associated with pyrimethamine resistance of Plasmodium falciparum
42. Structural specificity of chloroquine-hematin binding related to inhibition of hematin polymerization and parasite growth
43. Chloroquine-resistant malaria
44. A comparison of the antimalarial activity of the cinchona alkaloids against Plasmodium falciparum in vitro
45. Antimalarial drug resistance: The pace quickens