@article{fdi:010040851,
  title = {{A}ntifolate screening using yeast expressing {P}lasmodium vivax dihydrofolate reductase and in vitro drug susceptibility assay for {P}lasmodium falciparum},
  author = {{D}japa, {L}. {Y}. and {B}asco, {L}eonardo and {Z}elikson, {R}. and {R}osowsky, {A}. and {D}jaman, {J}. {A}. and {Y}onkeu, {J}. {N}. and {B}olotin {F}ukuhara, {M}. and {M}azabraud, {A}.},
  abstract = {{T}he presence of homologous point mutations in the dhfr gene in {P}lasmodium vivax and {P}lasmodium falciparum is associated with resistance to antifolate drugs. {T}he spread of antifolate resistance encouraged research for novel antifolate drugs active against both wild-type and dhfr-mutant strains of malaria parasites. {B}ecause {P}. vivax cannot be easily maintained in culture, we transformed a {S}accharomyces cerevisiae {DHFR}-deleted mutant to express wild-type {P}. vivax dhfr gene and its mutant forms. {T}wenty-five dicyclic and tricyclic 2,4-diaminopyrimidine derivatives were screened. {S}ix quinazoline compounds showed selective inhibition of yeast transformants expressing {R} vivax dhfr genes. {T}he 50% inhibitory concentration ({IC}50) of these six compounds was determined against field isolates of {P} falciparum. {O}ur results suggest that a close relationship between the yeast assay based on expression of {R} vivax dhfr genes and the in vitro test using {P} falciparum parasites in culture is a promising initial step for drug screening.},
  keywords = {antifolate drugs ; {P}lasmodium vivax ; {P}lasmodium falciparum in vitro culture ; malaria ; yeast ; drug resistance},
  journal = {{M}olecular and {B}iochemical {P}arasitology},
  volume = {156},
  numero = {1},
  pages = {89--92},
  ISSN = {0166-6851},
  year = {2007},
  DOI = {10.1016/j.molbiopara.2007.07.009},
  URL = {http://www.documentation.ird.fr/hor/fdi:010040851},
}