Literature summary for 1.5.1.33 extracted from

Cavazzuti, A.; Paglietti, G.; Hunter, W.N.; Gamarro, F.; Piras, S.; Loriga, M.; Allecca, S.; Corona, P.; McLuskey, K.; Tulloch, L.; Gibellini, F.; Ferrari, S.; Costi, M.P.
Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development (2008), Proc. Natl. Acad. Sci. USA, 105, 1448-1453.

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Application

Application	Comment	Organism
drug development	target for antiparasite drug development	Trypanosoma cruzi
drug development	target for antiparasite drug development	Leishmania major

Crystallization (Commentary)

Crystallization (Comment)	Organism
crystallized in complex with reduced cofactor and two different inhibitors	Leishmania major

Inhibitors

Inhibitors	Comment	Organism	Structure
(4S)-4-[[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]phenyl)carbonyl]amino]-5-oxohexanoic acid	-	Leishmania major
(4S)-4-[[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]phenyl)carbonyl]amino]-5-oxohexanoic acid	-	Trypanosoma cruzi
1-[(4-[[6-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-4-carboxylic acid	-	Leishmania major
1-[(4-[[6-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-4-carboxylic acid	-	Trypanosoma cruzi
1-[(4-[[8-amino-3-phenyl-6-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-4-carboxylic acid	-	Leishmania major
1-[(4-[[8-amino-3-phenyl-6-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-4-carboxylic acid	-	Trypanosoma cruzi
dimethyl 1-[(4-[[3-(ethoxycarbonyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2,4-dicarboxylate	-	Trypanosoma cruzi
dimethyl 1-[(4-[[3-phenyl-7-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2,4-dicarboxylate	-	Trypanosoma cruzi
ethyl 1-[(4-[[7-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2-carboxylate	-	Leishmania major
ethyl 1-[(4-[[7-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2-carboxylate	-	Trypanosoma cruzi
methyl 1-[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]phenyl)carbonyl]piperidine-4-carboxylate	-	Leishmania major
methyl 1-[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]phenyl)carbonyl]piperidine-4-carboxylate	-	Trypanosoma cruzi
methyl 1-[(4-[[(2,4-diaminopteridin-6-yl)methyl]amino]phenyl)carbonyl]piperidine-4-carboxylate	-	Leishmania major
methyl 1-[(4-[[(2,4-diaminopteridin-6-yl)methyl]amino]phenyl)carbonyl]piperidine-4-carboxylate	-	Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Trypanosoma cruzi	essential for the salvage of pterins	?	-	?
additional information	Leishmania major	essential for the salvage of pterins	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Leishmania major	Q01782	-	-
Trypanosoma cruzi	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	essential for the salvage of pterins	Trypanosoma cruzi	?	-	?
additional information	essential for the salvage of pterins	Leishmania major	?	-	?

Synonyms

Synonyms	Comment	Organism
pteridine reductase 1	-	Trypanosoma cruzi
pteridine reductase 1	-	Leishmania major
PTR1	-	Trypanosoma cruzi
PTR1	-	Leishmania major

Cofactor

Cofactor	Comment	Organism	Structure
NADPH	-	Trypanosoma cruzi
NADPH	-	Leishmania major

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000037	-	methyl 1-[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]phenyl)carbonyl]piperidine-4-carboxylate	-	Leishmania major
0.0001	-	methyl 1-[(4-[[(2,4-diaminopteridin-6-yl)methyl]amino]phenyl)carbonyl]piperidine-4-carboxylate	-	Leishmania major
0.00011	-	(4S)-4-[[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]phenyl)carbonyl]amino]-5-oxohexanoic acid	-	Trypanosoma cruzi
0.00018	-	(4S)-4-[[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]phenyl)carbonyl]amino]-5-oxohexanoic acid	-	Leishmania major
0.006	-	ethyl 1-[(4-[[7-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2-carboxylate	-	Leishmania major
0.007	-	1-[(4-[[6-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-4-carboxylic acid	-	Leishmania major
0.007	-	methyl 1-[(4-[[(2,4-diaminopteridin-6-yl)methyl]amino]phenyl)carbonyl]piperidine-4-carboxylate	-	Trypanosoma cruzi
0.02	-	1-[(4-[[8-amino-3-phenyl-6-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-4-carboxylic acid	-	Trypanosoma cruzi
0.038	-	dimethyl 1-[(4-[[3-(ethoxycarbonyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2,4-dicarboxylate	-	Trypanosoma cruzi
0.04	-	dimethyl 1-[(4-[[3-phenyl-7-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2,4-dicarboxylate	-	Trypanosoma cruzi
0.075	-	1-[(4-[[6-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-4-carboxylic acid	-	Trypanosoma cruzi
0.106	-	ethyl 1-[(4-[[7-(trifluoromethyl)quinoxalin-2-yl]amino]phenyl)carbonyl]piperidine-2-carboxylate	-	Trypanosoma cruzi

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Release 2023.1 (January 2023)