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Literature summary extracted from

  • Adane, L.; Patel, D.S.; Bharatam, P.V.
    Shape- and chemical feature-based 3D-pharmacophore model generation and virtual screening: identification of potential leads for P. falciparum DHFR enzyme inhibition (2009), Chem. Biol. Drug Des., 75, 115-126.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
1.5.1.3 A16V point mutation of the active site residue leads to a widespread resistance of the parasite to the drugs cycloguanil and pyrimethamine Plasmodium falciparum
1.5.1.3 C59R point mutation of the active site residue leads to a widespread resistance of the parasite to the drugs cycloguanil and pyrimethamine Plasmodium falciparum
1.5.1.3 I164X point mutation of the active site residue leads to a widespread resistance of the parasite to the drugs cycloguanil and pyrimethamine Plasmodium falciparum
1.5.1.3 N51I point mutation of the active site residue leads to a widespread resistance of the parasite to the drugs cycloguanil and pyrimethamine Plasmodium falciparum
1.5.1.3 S108N point mutation of the active site residue leads to a widespread resistance of the parasite to the drugs cycloguanil and pyrimethamine Plasmodium falciparum
1.5.1.3 S108T point mutation of the active site residue leads to a widespread resistance of the parasite to the drugs cycloguanil and pyrimethamine Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 Chloroquine
-
Plasmodium falciparum
1.5.1.3 cycloguanil an antifolate enzyme inhibitor used in treatment of malaria Plasmodium falciparum
1.5.1.3 additional information design and development of enzyme inhibitors based on on the bioactive conformation of WR99210 extracted from the X-ray crystal structure of quadruple mutant parasite DHFR enzyme, virtual screening and molecular docking, overview Plasmodium falciparum
1.5.1.3 NCI0086195 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0109835 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0156252 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0164641 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0211175 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0289533 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0289541 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0309401 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0369769 docking analysis, overview Plasmodium falciparum
1.5.1.3 NCI0696662 docking analysis, overview Plasmodium falciparum
1.5.1.3 pyrimethamine an antifolate enzyme inhibitor used in treatment of malaria Plasmodium falciparum
1.5.1.3 WR99210 docking analysis, overview Plasmodium falciparum

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Plasmodium falciparum
-
5,6,7,8-tetrahydrofolate + NADP+
-
r

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Plasmodium falciparum
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
1.5.1.3 5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ Ala16, Ile51, Cys59, Ser108 and Ile164 are active site residues Plasmodium falciparum

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
Plasmodium falciparum 5,6,7,8-tetrahydrofolate + NADP+
-
r

Synonyms

EC Number Synonyms Comment Organism
1.5.1.3 DHFR
-
Plasmodium falciparum

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADP+
-
Plasmodium falciparum
1.5.1.3 NADPH
-
Plasmodium falciparum