Basis for antifolate action and resistance in malaria

Microbes and Infection

Volumn 4, Issue 2, 2002, Pages 175-182

  Yuthavong, Yongyuth ^a  

^a NATIONAL SCIENCE AND TECHNOLOGY DEVELOPMENT AGENCY   (Thailand)

Author keywords

Antifolates; Malaria; Plasmodium falciparum; Resistance

Indexed keywords

4,6 DIAMINO 1,2 DIHYDRO 2,2 DIMETHYL 1 [3 (2,4,5 TRICHLOROPHENOXY)PROPOXY] 1,3,5 TRIAZINE; AMINO ACID; CHLORCYCLOGUANIL; CYCLOGUANIL; DAPSONE; DIHYDROFOLATE REDUCTASE; DIHYDROPTEROATE SYNTHASE; FOLIC ACID ANTAGONIST; METHOTREXATE; PYRIMETHAMINE; SULFADOXINE;

ANTIMALARIAL ACTIVITY; DRUG BINDING; DRUG DESIGN; DRUG EFFICACY; DRUG POTENTIATION; DRUG TARGETING; ENZYME ANALYSIS; ENZYME INHIBITION; ENZYME STRUCTURE; GENE MUTATION; HOST PARASITE INTERACTION; HUMAN; MALARIA FALCIPARUM; NONHUMAN; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; REVIEW;

ANIMALS; ANTIMALARIALS; DRUG COMBINATIONS; DRUG RESISTANCE; FOLIC ACID ANTAGONISTS; HUMANS; MALARIA; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PLASMODIUM FALCIPARUM; TETRAHYDROFOLATE DEHYDROGENASE;

PLASMODIUM FALCIPARUM;

EID: 0036185240     PISSN: 12864579     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1286-4579(01)01525-8     Document Type: Review

References (48)

1. Thymidylate synthase-dihydrofolate reductase in protozoa
2. An overview of chemotherapeutic targets for antimalarial drug discovery
3. Kinetic and molecular properties of dihydrofolate reductase from pyrimethamine-sensitive and pyrimethamine-resistant Plasmodium chabaudi
4. Amino acid changes linked to pyrimethamine resistance in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum
5. Evidence that a point mutation in dihydrofolate reductase-thymidylate synthase confers resistance to pyrimethamine in falciparum malaria
6. The dihydrofolate reductase-thymidylate synthase gene in the drug resistance of malaria parasites
7. Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those in pyrimethamine resistance
8. Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria
9. Transformation of Plasmodium falciparum malaria parasites by homologous integration of plasmids that confer resistance to pyrimethamine
10. Antifolate-resistant mutants of Plasmodium falciparum dihydrofolate reductase
11. Plasmodium falciparum: Asparagine mutant at residue 108 of dihydrofolate reductase is an optimal antifolate-resistant single mutant
12. Mutations in Plasmodium falciparum dihydrofolate reductase and dihydropteroate synthase and epidemiologic patterns of pyrimethamine-sulfadoxine use and resistance
13. Antifolate resistance due to new and known Plasmodium falciparum dihydrofolate reductase mutations expressed in yeast
14. Pyrimethamine resistant mutations in Plasmodium falciparum
15. Characterization of a cis-acting regulatory element in the protein coding region of thymidylate synthase mRNA
16. A biochemical and genetic model for parasite resistance to antifolates. Toxoplasma gondii provides insight into pyrimethamine and cycloguanil resistance in Plasmodium falciparum
17. Rational drug design approach for overcoming drug resistance: Application to pyrimethamine resistance in malaria
18. Lead discovery of inhibitors of the dihydrofolate reductase domain of Plasmodium falciparum dihydrofolate reductase-thymidylate synthase
19. Antimalarial drug discovery: Development of inhibitors of dihydrofolate reductase active in drug resistance
20. Towards an understanding of drug resistance in malaria: Three-dimensional structure of Plasmodium falciparum dihydrofolate reductase by homology building
21. Interaction of pyrimethamine, cycloguanil, WR99210, and their analogues with Plasmodium falciparum dihydrofolate reductase: Structural basis of antifolate resistance
22. Chemotherapy for falciparum malaria: The armory, the problems and the prospects
23. Treatment of Plasmodium falciparum malaria with pyrimethamine-silfadoxine: Selective pressure for resistance is a function of long elimination half life
24. Dihydrofolate reductase. The stereochemistry of inhibitor selectivity
25. Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil resistant strain (T9/94) of Plasmodium falciparum
26. Development of inhibitors for multiple mutants of dihydrofolate reductase from pyrimethamine-resistant Plasmodium falciparum
27. Treatment of Plasmodium falciparum malaria with pyrimethamine and sulfadoxine: A selective pressure for resistance in a function of long elimination half-life
28. The efficacy of antifolate antimalarial combinations in Africa: A predictive model based on pharmacodynamics and pharmacokinetic analyses
29. Synergism in the folate pathway
30. Antagonism of sulfadoxine and pyrimethamine antimalarial activities in vitro by p-aminobenzoic acid, p-aminobenzoylglutamic acid and folic acid
31. In vitro activities of and mechanisms of resistance to antifol antimalarial drugs
32. De novo and salvage biosynthesis of pteroylpentaglutamates in the human malaria parasite, Plasmodium falciparum
33. Sulfadoxine resistance in the human malaria parasite Plasmodium falciparum is determined by mutations in dihydropteroate synthetase and an additional factor associated with folate utilization
34. On 'the efficacy of antifolate antimalarial combinations in Africa'
35. Selection and synergy in Plasmodium falciparum
36. Utilization of exogenous folate in the human malaria parasite Plasmodium falciparum and its critical role in antifolate drug synergy
37. Sequence variation of the hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase genes in lines of the human malaria parasite, Plasmodium falciparum, with differing resistance to sulfadoxine
38. Mutations in dihydropteroate synthase are responsible for sulfone and sulfonamide resistance in Plasmodium falciparum
39. Resistance to antifolates in Plasmodium falciparum monitored by sequence analysis of dihydropteroate synthetase and dihydrofolate reductase alleles in a large number of field samples of diverse origins
40. Mutations in dihydropteroate synthase are responsible for sulfone and sulfonamide resistance in Plasmodium falciparum
41. More on 'the efficacy of antifolate antimalarial combinations in Africa'
42. Molecular basis of in vivo resistance to sulfadoxine-pyrimethamine in African adult patients infected with Plasmodium falciparum malaria parasites
43. Allelic exchange at the endogenous genomic locus in Plasmodium falciparum proves the role of dihydropteroate synthase in sulfadoxine-resistant malaria
44. Kenyan Plasmodium falciparum field isolates: Correlation between pyrimethamine and chlorcycloguanil activity in vitro and point mutations in the dihydrofolate reductase domain
45. Pyrimethamine-sulfadoxine efficacy and selection for mutations in Plasmodium falciparum dihydrofolate reductase and dihydropteroate synthase in Mali
46. Antibacterial synergism. A proposal for chemotherapeutic potentiation between trimethoprim and sulfamethoxazole
47. Potentiating effect of pyrimethamine and sulfadoxine against dihydrofolate reductase from pyrimethamine-sensitive and pyrimethamine-resistant Plasmodium chabaudi