Harnessing evolutionary fitness in Plasmodium falciparum for drug discovery and suppressing resistance

Proceedings of the National Academy of Sciences of the United States of America

Volumn 111, Issue 2, 2014, Pages 799-804

  Lukens, Amanda K ^a   Ross, Leila Saxby ^b   Heidebrecht, Richard ^a   Gamo, Francisco Javier ^c   Lafuente Monasterio, Maria J ^c   Booker, Michael L ^d   Hartl, Daniel L ^e   Wiegand, Roger C ^a   Wirth, Dyann F ^a,b  

^a BROAD INSTITUTE OF MIT AND HARVARD   (United States)

^b HARVARD SCHOOL OF PUBLIC HEALTH   (United States)

^c Glaxo SmithKline   (Spain)

^d GENZYME CORPORATION   (United States)

^e HARVARD UNIVERSITY   (United States)

Author keywords

Combination therapy; Evolution; Target identification

Indexed keywords

ANTIPROTOZOAL AGENT; ATOVAQUONE; CHLOROQUINE; CYCLOGUANIL; DIHYDROARTEMISININ; DIHYDROOROTATE DEHYDROGENASE; DSM 74; GENZ 666136; GSK 3; IDI 3783; MEFLOQUINE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ARTICLE; CONTROLLED STUDY; DRUG POTENCY; IN VITRO STUDY; MALARIA; MOLECULAR EVOLUTION; MUTANT; NONHUMAN; PLASMODIUM FALCIPARUM; POINT MUTATION; PRIORITY JOURNAL; WILD TYPE;

COMBINATION THERAPY; EVOLUTION; TARGET IDENTIFICATION;

ANALYSIS OF VARIANCE; BASE SEQUENCE; CHLOROQUINE; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; DRUG RESISTANCE; GENETIC FITNESS; GENOME; MALARIA; MOLECULAR SEQUENCE DATA; OXIDOREDUCTASES ACTING ON CH-CH GROUP DONORS; PLASMODIUM FALCIPARUM; POINT MUTATION; PYRIMIDINES; SEQUENCE ANALYSIS, DNA; SMALL MOLECULE LIBRARIES; TRIAZOLES;

EID: 84892582609     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1320886110     Document Type: Article

References (30)

1. World Health Organization (2011) World Malaria Report (World Health Organization, Geneva).
2. Dondorp AM, et al. (2009) Artemisinin resistance in Plasmodium falciparum malaria. N Engl J Med 361(5):455-467.
3. Costanzo MS, Hartl DL (2011) The evolutionary landscape of antifolate resistance in Plasmodium falciparum. J Genet 90(2):187-190.
4. Nzila A, Mwai L (2010) In vitro selection of Plasmodium falciparum drug-resistant parasite lines. J Antimicrob Chemother 65(3):390-398.
5. Sarafianos SG, Das K, Hughes SH, Arnold E (2004) Taking aim at a moving target: Designing drugs to inhibit drug-resistant HIV-1 reverse transcriptases. Curr Opin Struct Biol 14(6):716-730.
6. Shah NP, et al. (2002) Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2(2):117-125.
7. Quintás-Cardama A, Kantarjian H, Cortes J (2007) Flying under the radar: The new wave of BCR-ABL inhibitors. Nat Rev Drug Discov 6(10):834-848.
8. Wootton JC, et al. (2002) Genetic diversity and chloroquine selective sweeps in Plasmodium falciparum. Nature 418(6895):320-323.
9. Laufer MK, et al. (2006) Return of chloroquine antimalarial efficacy in Malawi. N Engl J Med 355(19):1959-1966.
10. Martin SK, Oduola AM, Milhous WK (1987) Reversal of chloroquine resistance in Plasmodium falciparum by verapamil. Science 235(4791):899-901.
11. Martiney JA, Cerami A, Slater AF (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(38):22393-22398.
12. Martin RE, et al. (2009) Chloroquine transport via the malaria parasite?s chloroquine resistance transporter. Science 325(5948):1680-1682.
13. Ye ZG, Van Dyke K (1988) Reversal of chloroquine resistance in falciparum malaria independent of calcium channels. Biochem Biophys Res Commun 155(1):476-481.
14. Bruce-Chwatt LJ (1982) Chemoprophylaxis of malaria in Africa: The spent ?magic bullet?. Br Med J (Clin Res Ed) 285(6343):674-676.
15. Hurt DE, Widom J, Clardy J (2006) Structure of Plasmodium falciparum dihydroorotate dehydrogenase with a bound inhibitor. Acta Crystallogr D Biol Crystallogr 62(Pt 3): 312-323.
16. Booker ML, et al. (2010) Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model. J Biol Chem 285(43): 33054-33064.
17. Phillips MA, Rathod PK (2010) Plasmodium dihydroorotate dehydrogenase: A promising target for novel anti-malarial chemotherapy. Infect Disord Drug Targets 10(3): 226-239.
18. Fidock DA, et al. (2000) Mutations in the P. falciparum digestive vacuole transmembrane protein PfCRT and evidence for their role in chloroquine resistance. Mol Cell 6(4):861-871.
19. Skerlj RT, et al. (2011) Optimization of potent inhibitors of P. falciparum dihydroorotate dehydrogenase for the treatment of malaria. ACS Medicinal Chem Lett 2(9): 708-713.
20. Gujjar R, et al. (2009) Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice. J Med Chem 52(7):1864-1872.
21. Phillips MA, et al. (2008) Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum. J Med Chem 51(12):3649-3653.
22. Malmquist NA, Gujjar R, Rathod PK, Phillips MA (2008) Analysis of flavin oxidation and electron-transfer inhibition in Plasmodium falciparum dihydroorotate dehydrogenase. Biochemistry 47(8):2466-2475.
23. Bollenbach T, Quan S, Chait R, Kishony R (2009) Nonoptimal microbial response to antibiotics underlies suppressive drug interactions. Cell 139(4):707-718.
24. Edwards MJ, et al. (2009) A crystal structure of the bifunctional antibiotic simocyclinone D8, bound to DNA gyrase. Science 326(5958):1415-1418.
25. Aurrecoechea C, et al. (2009) PlasmoDB: A functional genomic database for malaria parasites. Nucleic Acids Res 37(Database issue):D539-D543.
26. DePristo MA, et al. (2011) A framework for variation discovery and genotyping using next-generation DNA sequencing data. Nat Genet 43(5):491-498.
27. Li H, et al.; 1000 Genome Project Data Processing Subgroup (2009) The sequence alignment/map format and SAMtools. Bioinformatics 25(16):2078-2079.
28. Johnson JD, et al. (2007) Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening. Antimicrob Agents Chemother 51(6):1926-1933.
29. Fivelman QL, Adagu IS, Warhurst DC (2004) Modified fixed-ratio isobologram method for studying in vitro interactions between atovaquone and proguanil or dihydroartemisinin against drug-resistant strains of Plasmodium falciparum. Antimicrob Agents Chemother 48(11):4097-4102.
30. McNicholas S, Potterton E, Wilson KS, Noble ME (2011) Presenting your structures: The CCP4mg molecular-graphics software. Acta Crystallogr D Biol Crystallogr 67(Pt 4): 386-394.