Biochemical and genetic tests for inhibitors of Leishmania pteridine pathways

Experimental Parasitology

Volumn 87, Issue 3, 1997, Pages 157-169

  Hardy, L W ^a   Matthews, W ^a   Nare, B ^b,c   Beverley, S M ^b,d  

^a UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c MERCK RESEARCH LABORATORIES   (United States)

^d WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DIHYDROFOLIC ACID; FOLIC ACID ANTAGONIST; PTERIDINE;

ARTICLE; CONTROLLED STUDY; DRUG TARGETING; GENE AMPLIFICATION; GENETIC ANALYSIS; LEISHMANIA; LEISHMANIA MAJOR; METABOLISM; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; CELL DIVISION; DRUG RESISTANCE; FOLIC ACID ANTAGONISTS; HUMANS; LEISHMANIA; METHOTREXATE; MICROBIAL SENSITIVITY TESTS; MULTIENZYME COMPLEXES; MUTATION; OXIDOREDUCTASES; PTERIDINES; PYRIMIDINES; QUINAZOLINES; SPECIES SPECIFICITY; TETRAHYDROFOLATE DEHYDROGENASE; THYMIDYLATE SYNTHASE;

EUKARYOTA; LEISHMANIA MAJOR; PROTOZOA;

EID: 0031282556     PISSN: 00144894     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. Baldwin, S. W., Tse, A., Gossett, L. S., Taylor, E. C., Rosowsky, A., Shih, C., and Moran, R. G. 1991. Structural features of 5,10-dideaza-5,6,7,8-tetrahydrofolate that determine inhibition of mammalian glycinamide ribonucleotide formyltransferase. Biochemistry 30, 1997-2006.
2. Bello, A. R., Nare, B., Freedman, D., Hardy, L. W., and Beverley, S. M. 1994. PTR1: A reductase mediating salvage of oxidized pteridines and methotrexate resistance in the protozoan parasite Leishmania major. Proceedings of the National Academy of Sciences USA 91, 11442-11446.
3. Berman, J. D., King, M., and Edwards, N. 1989. Antileishmanial activities of 2,4-diaminoquinazoline putative dihydrofolate reductase inhibitors. Antimicrobial Agents and Chemotherapy 33, 1860-1863.
4. Beverley, S. M. 1991. Gene amplification in Leishmania. Annual Review of Microbiology 45, 417-444.
5. Beverley, S. M., Coderre, J. A., Santi, D. V., and Schimke, R. T. 1984. Unstable DNA amplifications in methotrexate resistant Leishmania consist of extrachromosomal circles which relocate during stabilization. Cell 38, 431-439.
6. Borst, P., and Ouellette, M. 1995. New mechanisms of drug resistance in parasitic protozoa. Annual Review of Microbiology 49, 427-460.
7. Callahan, H. L., and Beverley, S. M. 1992. A member of the aldoketo reductase family confers resistance to methotrexate in Leishmania. Journal of Biological Chemistry 267, 24165-24168.
8. Cha, S. 1975. Tight-binding inhibitors. I. Kinetic behavior. Biochemical Pharmacology 24, 2177-2185.
9. Coderre, J. A., Beverley, S. M., Schimke, R. T., and Santi, D. V. 1983. Overproduction of a bifunctional dihydrofolate reductase-thymidylate synthase and DNA amplification in methotrexate-resistant Leishmania tropica. Proceedings of the National Academy of Sciences USA 80, 2132-2136.
10. Cruz, A., and Beverley, S. M. 1990. Gene replacement in parasitic protozoa. Nature 348, 171-173.
11. Cruz, A., Coburn, C. M., and Beverley, S. M. 1991. Double gene replacement for creating null mutants. Proceedings of the National Academy of Sciences USA 88, 7170-7174.
12. Dews, H., Ostergaard, H., and Simpson, L. 1986. Impaired drug uptake in methotrexate resistant Crithidia fasticulata without change in dihydrofolate reductase activity or gene amplification. Molecular and Biochemical Pharmacology 19, 149-161.
13. Ellenberger, T. E., and Beverley, S. M. 1987a. Biochemistry and regulation of folate and methotrexate transport in Leishmania major. Journal of Biological Chemistry 262, 10053-10058.
14. Ellenberger, T. E., and Beverley, S. M. 1987b. Reductions in methotrexate and folate influx in methotrexate-resistant lines of Leishmania major are independent of R and H-region amplification. Journal of Biological Chemistry 262, 13501-13506.
15. Ferone, R. 1984. Dihydrofolate inhibitors. In "Antimalarial Drugs. Vol. II. The Handbook of Experimental Parasitology." (W. Peter and W. H. G. Richards, Eds.), Vol. 68, pp. 207-221. Springer-Verlag, New York.
16. Grossman, P. L., and Remington, J. S. 1979. The effect of trimethoprim and sulfamethazole on Toxoplasma gondii in vitro and in vivo. American Journal of Tropical Medicine and Hygiene 28, 445-455.
17. Gueiros-Filho, F. J., and Beverley, S. M. 1996. Selection against the dihydrofolate reductase-thymidylate synthase (DHFR-TS) locus as a probe of genetic alterations in Leishmania major. Molecular and Cellular Biology 16, 5655-5663.
18. Hynes, J. B., Eason, D. E., Garrett, C. M., and Colvin, P. L., Jr. 1977. Quinazolines as inhibitors of dihydrofolate reductase. 4. Classical analogues of folic and isofolic acids. Journal of Medicinal Chemistry 20, 588-591.
19. Ivanetich, K. M., and Santi, D. V. 1990. Bifunctional thymidylate synthase-dihydrofolate reductase in protozoa. FASEB Journal 4, 1591-1597.
20. Janin, J., van Rapenbusch, R., Truffa-Bachi, P., and Cohen, G. N. 1969. The threonine-sensitive homoserine dehydrogenase and aspartokinase activities of Escherichia coli K12: Binding of threonine and of pyridine nucleotides: stoichiometry and optical effects. European Journal of Biochemistry 8, 128-138.
21. Kapler, G. M., Coburn, C. M., and Beverley, S. M. 1990. Stable transfection of the human parasite Leishmania major delineates a 30-kilobase region sufficient for extrachromosomal replication and expression. Molecular and Cellular Biology 10, 1084-1094.
22. Kaur, K., Coons, T., Emmett, K., and Ullman, B. 1988. Methotrexate-resistant Leishmania donovani genetically deficient in the folate-methotrexate transporter. Journal of Biological Chemistry 263, 7020-7028.
23. Kiefer, P. M., Varughese, K. L., Su, Y., Xuong, N.-H., Chang, C.-F., Gupta, P., Bray, T., and Whiteley, J. M. 1996. Altered structural and mechanistic properties of mutant dihydropteridine reductases. Journal of Biological Chemistry 271, 3437-3444.
24. McDougald, L. R. 1982. Chemotherapy of coccidiosis. In "The Biology of the Coccidia" (P. L. Long, Ed.), pp. 373-428. Univ. Park Press, Baltimore.
25. Nare, B., Hardy, L., and Beverley, S. M. 1997a. The roles of pteridine reductase 1 and dihydrofolate reductase-thymidylate synthase in pteridine metabolism in the protozoan parasite Leishmania major. Journal of Biological Chemistry 272, 13883-13891.
26. Nare, B., Luba, J., Hardy, L. W., and Beverley, S. M. 1997b. New approaches to Leishmania chemotherapy: Pteridine reductase 1 (PTR1) as a target and modulator of antifolate sensitivity. Parasitology. [in press]
27. Papadopoulou, B., Roy, G., and Ouellette, M. 1992. A novel antifolate resistance gene on the amplified H circle of Leishmania. The EMBO Journal 11, 3601-3608.
28. Papadopoulou, B., Roy, G., Mourad, W., Leblanc, E., and Ouellette, M. 1994. Changes in folate and pterin metabolism after disruption of the Leishmania H locus short chain dehydrogenase gene. Journal of Biological Chemistry 269, 7310-7318.
29. Prendergast, N. J., Delcamp, T. J., Smith, P. L., and Freisheim, J. H. 1988. Expression and site-directed mutagenesis of human dihydrofolate reductase. Biochemistry 27, 3664-3671.
30. Scanlon, K. J., Moroson, B. A., Bertino, J. R., and Hynes, J. B. 1979. Quinazoline analogues of folic acid as inhibitors of thymidylate synthetase from bacterial and mammalian sources. Molecular Pharmacology 16, 261-269.
31. Scott, D. A., Coombs, G. H., and Sanderson, B. E. 1987a. Effects of methotrexate and other antifolates on the growth and dihydrofolate reductase activity of Leishmania promastigotes. Biochemical Pharmacology 36, 2043-2045.
32. Scott, D. A., Coombs, G. H., and Sanderson, B. E. 1987b. Folate utilization by Leishmania species and the identification of intracellular derivatives and folate-metabolising enzymes. Molecular and Biochemical Pharmacology 23, 139-149.
33. Shih, C., Chen, V. J., Gossett, L. S., Gates, S. B., MacKellar, W. C., Habeck, L. L., Shackelford, K. A., Mendelsohn, L. G., Soose, D. J., Patel, V. F., Andis, S. L., Bewley, J. R., Rayl, E. A., Moroson, B. A., Beardsley, G. P., Kohler, W., Ratnam, M., and Schultz, R. M. 1997. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Research 57, 1116-1123.
34. Sirawaraporn, W., Sertsrivanich, R., Booth, R. G., Mansch, C., Neal, R. A., and Santi, D. V. 1988. Selective inhibition of Leishmania dihydrofolate reductase and Leishmania growth by 5-benzyl-2,4-diaminopyrimidines. Molecular and Biochemical Parasitology 31, 79-86.