Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.5.1.15 extracted from

  • Berglez, J.; Iliades, P.; Sirawaraporn, W.; Coloe, P.; Macreadie, I.
    Analysis in Escherichia coli of Plasmodium falciparum dihydropteroate synthase (DHPS) alleles implicated in resistance to sulfadoxine (2004), Int. J. Parasitol., 34, 95-100.
    View publication on PubMed
Search for more literature for 2.5.1.15

Protein Variants

Protein Variants Comment Organism
A437G mutant enzyme is resistant against inhibition by sulfadoxine and sulfpyridine (inhibitors of wild-type enzyme) Plasmodium falciparum
A437G/A581G mutant enzyme is resistant against inhibition by sulfadoxine, sulfpyridine, sulfadimethoxine, sulfamethoxazole, sulfaquinoxaline and sulfisoxazole (inhibitors of wild-type enzyme) Plasmodium falciparum
A437G/K540E sulfadoxine, sulfpyridine, sulfadimethoxine, sulfamethoxazole, sulfaquinoxaline, sulfisoxazole, sulfanilamide, sulfamerazine, sulfathiazole, dapsone, sulfamoxisole, sulfachloropyridazine and sulfacetamide (inhibitors of wild-type enzyme) Plasmodium falciparum
S436F/A437G/A613S sulfadoxine, sulfpyridine, sulfadimethoxine, sulfamethoxazole, sulfaquinoxaline, sulfisoxazole, sulfanilamide, sulfamerazine, sulfathiazole and dapsone (inhibitors of wild-type enzyme) Plasmodium falciparum
S436F/A437G/A613T sulfadoxine, sulfpyridine, sulfadimethoxine, sulfamethoxazole, sulfaquinoxaline, sulfisoxazole, sulfanilamide, sulfamerazine, sulfathiazole and dapsone (inhibitors of wild-type enzyme) Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
dapsone effective against wild-type enzyme and mutants A437G/K540E and A437G. Ineffective against mutants A437G/A581G, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfacetamide effective against wild-type enzyme and mutant enzymes A437G/K540E, A437G, A437G/A581G, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfachloropyridazine effective against wild-type enzyme and mutant enzymes A437G/K540E, A437G, A437G/A581G, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfadimethoxine effective against wild-type enzyme and mutant A437G. Ineffective against mutants A437G/A581G, A437G/K540E, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfadoxine effective against wild-type enzyme. Ineffective against mutants A437G, A437G/A581G, A437G/K540E, S436F/A437G/A613S and S436F/A437G/A613T. IC50 for wild-type enzyme: 0.071 mg/ml, IC50 for mutant enzyme A437G: 0.203 mg/ml, IC50 for mutant enzyme A437G/K540E: 0.423 mg/ml, IC50 for mutant enzyme A437G/A581G: 0.775 mg/ml, IC50 for mutant enzymes S436F/A437G/A613S and S436F/A437G/A613T is above 1 mg/ml Plasmodium falciparum
sulfamerazine effective against wild-type enzyme and mutants A437G/K540E and A437G. Ineffective against mutants A437G/A581G, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfamethoxazole effective against wild-type enzyme and mutant A437G. Ineffective against mutants A437G/A581G, A437G/K540E, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfamoxisole effective against wild-type enzyme and mutant enzymes A437G/K540E, A437G, S436F/A437G/A613S and S436F/A437G/A613T. Ineffective against A437G/A581G Plasmodium falciparum
sulfanilamide effective against wild-type enzyme and mutants A437G/K540E and A437G. Ineffective against mutants A437G/A581G, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfaquinoxaline effective against wild-type enzyme and mutant A437G. Ineffective against mutants A437G/A581G, A437G/K540E, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfathiazole effective against wild-type enzyme and mutants A437G/K540E and A437G. Ineffective against mutants A437G/A581G, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfisoxazole effective against wild-type enzyme and mutant A437G. Ineffective against mutants A437G/A581G, A437G/K540E, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum
sulfpyridine effective against wild-type enzyme. Ineffective against mutants A437G, A437G/A581G, A437G/K540E, S436F/A437G/A613S and S436F/A437G/A613T Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-