Literature summary for 1.5.1.3 extracted from

Kongsaeree, P.; Khongsuk, P.; Leartsakulpanich, U.; Chitnumsub, P.; Tarnchompoo, B.; Walkinshaw, M.D.; Yuthavong, Y.
Crystal structure of dihydrofolate reductase from Plasmodium vivax: pyrimethamine displacement linked with mutation-induced resistance (2005), Proc. Natl. Acad. Sci. USA, 102, 13046-13051.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
wild-type and pyrimethamine-resistant mutant S58R/S117N in complex with NADPH and inhibitors pyrimethamine or 6-ethyl-5-phenylpyrimidine-2,4-diamine	Plasmodium vivax

Protein Variants

Protein Variants	Comment	Organism
S58R/S117N	pyrimethamine-resistant mutant	Plasmodium vivax

Inhibitors

Inhibitors	Comment	Organism	Structure
6-ethyl-5-phenylpyrimidine-2,4-diamine	analogue of pyrimethamine lacking the 4-Cl group, effectively inhibits both wild-type and pyrimethamine-resistant mutant S58R/S117N	Plasmodium vivax
pyrimethamine	-	Plasmodium vivax

Organism

Organism	UniProt	Comment	Textmining
Plasmodium vivax	O02604	-	-

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.00000016	-	pyrimethamine	wild-type	Plasmodium vivax
0.00000155	-	6-ethyl-5-phenylpyrimidine-2,4-diamine	wild-type	Plasmodium vivax
0.00000733	-	6-ethyl-5-phenylpyrimidine-2,4-diamine	mutant S58R/S117N	Plasmodium vivax
0.00005	-	pyrimethamine	mutant S58R/S117N	Plasmodium vivax

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Release 2023.1 (January 2023)