Access to hematin: The basis of chloroquine resistance

Molecular Pharmacology

Volumn 54, Issue 1, 1998, Pages 170-179

  Bray, Patrick G ^a   Mungthin, Mathirut ^a   Ridley, Robert G ^b   Ward, Stephen A ^a  

^a UNIVERSITY OF LIVERPOOL   (United Kingdom)

^b F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

AMODIAQUINE; CHLOROQUINE; DAUNORUBICIN; HEMATIN; PRIMAQUINE; VERAPAMIL;

ANTIMALARIAL ACTIVITY; ARTICLE; DRUG PROTEIN BINDING; DRUG RESISTANCE; ERYTHROCYTE; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; PROTON SODIUM EXCHANGE;

EID: 0031818645     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.54.1.170     Document Type: Article

References (45)

1. Balasubramanian D, Mohan Rao C, and Panjipan B (1984) The malaria parasite monitored by photoacoustic spectroscopy. Science (Washington DC) 223:828-830.
2. + antiport of Plasmodium falciparum membrane. J Cell Physiol 154:527-534.
3. Bray PG, Boulter MK, Ritchie GY, and Ward SA (1994) Relationship of global chloroquine transport and reversal of resistance in Plasmodium falciparum. Mol Biochem Parasitol 63:87-94.
4. Bray PG, Hawley SR, Mungthin M, and Ward SA (1996) Physicochemical properties correlated with drug resistance and the reversal of drug resistance in Plasmodium falciparum. Mol Pharmacol 50:1559-1566.
5. Bray PG, Howells RE, Ritchie GY, and Ward SA (1992a) Rapid chloroquine efflux phenotype in both chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum: a correlation of chloroquine sensitivity with energy-dependent drug accumulation. Biochem Pharmacol 44:1317-1324.
6. Bray PG, Howells RE, and Ward S (1992b) Vacuolar acidification and chloroquine sensitivity in Plasmodium falciparum. Biochem Pharmacol 43:1219-1227.
7. Chou AC, Chevli R, and Fitch CD (1980) Ferriprotoporphyrin IX fulfils the criteria for identification as the chloroquine receptor of malaria parasites. Biochemistry 19:1543.
8. De D, Krogstad FM, Cogswell FB, and Krogstad DJ (1996) Aminoquinolines that circumvent chloroquine resistance in Plasmodium falciparum. Am J Trop Med Hyg 55:579-583.
9. Desjardins RE, Canfield J, Haynes D, and Chulay JD (1979) Quantitative assessment of antimalarial activity in vitro by a semi-automated microdilution technique. Antimicrob Agents Chemother 16:710-718.
10. Dorn A, Stoffel R, Matile H, Bubendorf A, and Ridley RG (1995) Malarial haemozoin beta-haematin supports haeme polymerization in the absence of protein. Nature (Lond) 374:269-271.
11. Dorn A, Vippagunta SR, Matile H, Bubendorf A, Vennerstrom JL, and Ridley RG (1998) A comparison and analysis of several ways to promote hematin (heme) polymerisation and an assessment of its initiation in vitro. Biochem Pharmacol 55:737-747.
12. Ferrari V and Cutler DJ (1991) Simulation of kinetic data on the influx and efflux of chloroquine by erythrocytes infected with Plasmodium falciparum: evidence for a drug-importer in chloroquine-sensitive strains. Biochem Pharmacol 42:S167-S179.
13. Fitch CD (1970) Plasmodium falciparum in owl monkeys: drug resistance and chloroquine binding capacity. Science (Washington DC) 169:289-290.
14. Fitch CD (1989) Malaria and the Red Cell 2. pp 45-52, Alan R. Liss, New York.
15. Fitch CD and Chevli R (1981) Sequestration of the chloroquine receptor in cell-free preparations of erythrocytes infected with Plasmodium berghei. Antimicrob Agents Chemother 19:589-592.
16. Francis SE, Gluzman IY, Oksman A, Knickerbocker A, Mueller R, Bryant ML, Sherman DR, Russell DG, and Goldberg DE (1994) Molecular characterization and inhibition of a Plasmodium falciparum aspartic hemoglobinase. EMBO J 13:306-317.
17. Gabay T, Krugliak M, Shalmiev G, and Ginsburg H (1994) Inhibition by antimalarial drugs of haemoglobin denaturation and iron release in acidified erythrocytes: possible mechanism of their antimalarial effect. Parasitology 108:371-381.
18. Geary TG, Divo AD, Jensen JB, Zangwill M, and Ginsburg H (1990) Kinetic modeling of the response of Plasmodium falciparum to chloroquine and its experimental testing in vitro: implications for mechanism of action of and resistance to the drug. Biochem Pharmacol 40:685-691.
19. Ginsburg H and Geary TG (1987) Current concepts and new ideas on the mechanism of action of quinoline-containing antimalarials. Biochem Pharmacol 36:1567-1576.
20. Ginsburg H and Stein WD (1991) Kinetic modeling of chloroquine uptake by malariainfected erythrocytes: assessment of the factors that may determine drugresistance. Biochem Pharmacol 41:1463-1470.
21. Ginsburg H, Nissani E, and Krugliak M (1989) Alkalinization of the food vacuole of malaria parasites by quinoline drugs and alkylamines is not correlated with their antimalarial activity. Biochem Pharmacol 38:2645-2654.
22. Gluzman IY, Francis SE, Oksman A, Smith CE, Duffin KL, and Goldberg DE (1994) Order and specificity of the Plasmodium falciparum hemoglobin degradation pathway. J Clin Invest 93:1602-1608.
23. Hawley SR, Bray PG, O'Neill PM, Park BK, and Ward SA (1996a) The role of drug accumulation in 4-aminoquinoline antimalarial potency: the influence of structural substitution and physicochemical properties. Biochem Pharmacol 52:723-733.
24. Hawley SR, Bray PG, O'Neill PM, Naisbitt DJ, Park BK and Ward SA (1996b) Manipulation of the n-alkyl substituent in amodiaquine to overcome the verapamil-sensitive chloroquine resistance component. Antimicrob Agents Chemother 40:2345-2349.
25. Hawley SR, Bray PG, Park BK, and Ward SA (1996c) Amodiaquine accumulation in Plasmodium falciparum as a possible explanation for its superior antimalarial activity over chloroquine. Mol Biochem Parasitol 80:15-25.
26. Krogstad DJ, Gluzman IY, Kyle DE, Oduola AMJ, Martin SK, Milhous WK, and Schlesinger PH (1987) Efflux of chloroquine from Plasmodium falciparum: mechanism of chloroquine resistance. Science (Washington DC) 235:1283-1285.
27. Krogstad DJ, Schlesinger PH, and Gluzman IY (1985) Antimalarials increase vesicle pH in Plasmodium falciparum. J Cell Biol 101:2302-2309.
28. Macomber PB, Sprinz H, and Tousimis AJ (1967) Morphological effects of chloroquine on Plasmodium berghei in mice. Nature (Lond) 214:937-939.
29. Martiney JA, Cerami A, and Slater AFG (1995) Verapamil reversal of chloroquine resistance in the malaria parasite Plasmodium falciparum is specific for resistant parasites and independent of the weak base effect. J Biol Chem 270:22393-22398.
30. Menting JGT, Tilley L, Deady LW, Ng K, Simpson RJ, Cowman AF, and Foley M (1997) The antimalarial drug, chloroquine, interacts with lactate dehydrogenase from Plasmodium falciparum. Mol Biochem Parasitol 88:215-224.
31. Meshnick S (1996) Is haemozoin a target for antimalarial drugs? Ann Trop Med Parasitol 90:367-372.
32. Moon RP, Tyas L, Certa U, Rupp K, Bur D, Jacquet C, Matile H, Loetscher H, Grueninger-Leitch F, Kay J, Dunn BM, Berry C, and Ridley RG (1997) Expression and characterisation of plasmepsin I from Plasmodium falciparum. Eur J Biochem 244:552-560.
33. Ridley RG, Hofheinz W, Matile H, Jacquet C, Dorn A, Masciadri R, Jolidon S, Richter WF, Guenzi A, Girometta MA, Urwyler H, Huber W, Thaithong S, and Peters W (1996) 4-Aminoquinoline analogs of chloroquine with shortened side-chains retain activity against chloroquine-resistant Plasmodium falciparum. Antimicrob Agents Chemother 40:1846-1854.
34. Ridley RG, Dorn A, Vippagunta SR, and Vennerstrom, JL (1997) Haematin (haem) polymerisation and its inhibition by quinoline antimalarials. Ann Trop Med Parasitol 91:559-566.
35. Roberts DV (1977) Simple enzyme catalysed reactions, in Enzyme Kinetics (Elmore DT, Leadbetter AJ, and Schofield K, eds) Cambridge University Press, Cambridge, UK.
36. Sanchez CP, Wünsch S, and Lanzer M (1997) Identification of a chloroquine importer in Plasmodium falciparum: differences in import kinetics are genetically linked with the chloroquine-resistant phenotype. J Biol Chem 272:2652-2658.
37. Slater AFG (1993) Chloroquine: mechanism of drug-action and resistance in Plasmodium falciparum. Pharmacol Ther 57:203-235.
38. Su X, Kirkman LA, Fujioka H, and Wellems TE (1997) Complex polymorphisms in an ∼330 kDa protein are linked to chloroquine-resistant P. falciparum in Southeast Asia and Africa. Cell 91:593-603.
39. Sugioka Y and Suzuki M (1991) The chemical basis for the ferriprotoporphyrin IX-chloroquine complex induced lipid peroxidation. Biochim et Biophys Acta 1074:19-24.
40. Sullivan DJ Jr, Gluzman IY, Russell DG, and Goldberg DE (1996) On the molecular mechanism of chloroquine's antimalarial action. Proc Natl Acad Sci USA 93:11865-11870.
41. Vander Jagt DL, Hunsaker LA, and Campos NM (1987) Comparison of proteases from chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Biochem Pharmacol 36:3285-3291.
42. Warhurst DC (1986) Antimalarial schizontocides: why a permease is necessary. Parasitol Today 2:331-334.
43. Wellems TE, Walker-Jonah A, and Panton LJ (1991) Genetic mapping of the chloroquine resistance locus on Plasmodium falciparum chromosome 7. Proc Natl Acad Sci USA 88:3382-3386.
44. + exchanger determines chloroquine uptake in Plasmodium falciparum. J Cell Biol 140:335-345.
45. Yayon A, Cabantchik ZI, and Ginsburg H (1985) Susceptibility of human malaria parasites to chloroquine is pH dependent. Proc Natl Acad Sci USA 82:2784-2788.