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Literature summary extracted from

  • Zhang, Y.; Evans, G.B.; Clinch, K.; Crump, D.R.; Harris, L.D.; Froehlich, R.F.; Tyler, P.C.; Hazleton, K.Z.; Cassera, M.B.; Schramm, V.L.
    Transition state analogues of Plasmodium falciparum and human orotate phosphoribosyltransferases (2013), J. Biol. Chem., 288, 34746-34754.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.10 expressed in Escherichia coli Homo sapiens
2.4.2.10 expressed in Escherichia coli Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.10 (1R,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[(4-nitrophenyl)methyl]pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (1R,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[(4-nitrophenyl)methyl]pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (1S,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[2-(4-nitrophenyl)ethyl]pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (1S,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[2-(4-nitrophenyl)ethyl]pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (2R,3R,4S)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (2R,3R,4S)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (2R,3R,4S)-1-[2-(6-carboxy-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (2R,3R,4S)-1-[2-(6-carboxy-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (2R,3S)-3-hydroxy-2-(hydroxymethyl)-5-(4-nitrophenyl)pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (2R,3S)-3-hydroxy-2-(hydroxymethyl)-5-(4-nitrophenyl)pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (2S,3S,4R,5R)-2-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (2S,3S,4R,5R)-2-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (2S,3S,4R,5R)-2-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (2S,3S,4R,5R)-2-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (3R,4R)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 (3R,4R)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 (7R,8R,9S,9aS)-8,9-dihydroxy-7-(hydroxymethyl)-8,9,9a,10-tetrahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidine-1,3,5(2H)-trione
-
 Homo sapiens
2.4.2.10 (7R,8R,9S,9aS)-8,9-dihydroxy-7-(hydroxymethyl)-8,9,9a,10-tetrahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidine-1,3,5(2H)-trione
-
 Plasmodium falciparum
2.4.2.10 1,3-dihydroxy-N-[(4-nitrophenyl)methyl]propan-2-aminium
-
 Homo sapiens
2.4.2.10 1,3-dihydroxy-N-[(4-nitrophenyl)methyl]propan-2-aminium
-
 Plasmodium falciparum
2.4.2.10 1,3-dihydroxy-N-[2-(4-nitrophenyl)ethyl]propan-2-aminium
-
 Homo sapiens
2.4.2.10 1,3-dihydroxy-N-[2-(4-nitrophenyl)ethyl]propan-2-aminium
-
 Plasmodium falciparum
2.4.2.10 1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]pyrrolidin-1-ium
-
 Homo sapiens
2.4.2.10 1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]pyrrolidin-1-ium
-
 Plasmodium falciparum
2.4.2.10 4-nitrophenyl beta-D-ribose
-
 Homo sapiens
2.4.2.10 4-nitrophenyl beta-D-ribose
-
 Plasmodium falciparum
2.4.2.10 4-nitrophenyl beta-D-ribose 5'-phosphate
-
 Homo sapiens
2.4.2.10 4-nitrophenyl beta-D-ribose 5'-phosphate
-
 Plasmodium falciparum
2.4.2.10 [(2R,3R,4S,5S)-5-(4-carboxypyridin-3-yl)-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate
-
 Homo sapiens
2.4.2.10 [(2R,3R,4S,5S)-5-(4-carboxypyridin-3-yl)-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate
-
 Plasmodium falciparum
2.4.2.10 [(2R,3R,4S,5S)-5-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate
-
 Homo sapiens
2.4.2.10 [(2R,3R,4S,5S)-5-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate
-
 Plasmodium falciparum
2.4.2.10 [(2R,3R,4S,5S)-5-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate
-
 Homo sapiens
2.4.2.10 [(2R,3R,4S,5S)-5-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate
-
 Plasmodium falciparum
2.4.2.10 [(3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-4-hydroxypyrrolidin-1-ium-3-yl]methyl hydrogen phosphate
-
 Homo sapiens
2.4.2.10 [(3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-4-hydroxypyrrolidin-1-ium-3-yl]methyl hydrogen phosphate
-
 Plasmodium falciparum
2.4.2.10 [(7R,8R,9S,9aS)-8,9-dihydroxy-1,3,5-trioxo-1,2,3,5,8,9,9a,10-octahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidin-7-yl]methyl hydrogen phosphate
-
 Homo sapiens
2.4.2.10 [(7R,8R,9S,9aS)-8,9-dihydroxy-1,3,5-trioxo-1,2,3,5,8,9,9a,10-octahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidin-7-yl]methyl hydrogen phosphate
-
 Plasmodium falciparum

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.10 orotate + 5-phospho-alpha-D-ribose 1-diphosphate Homo sapiens
-
 orotidine 5'-phosphate + diphosphate
-
 ?
2.4.2.10 orotate + 5-phospho-alpha-D-ribose 1-diphosphate Plasmodium falciparum
-
 orotidine 5'-phosphate + diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.10 Homo sapiens
-
-
-
2.4.2.10 Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.10 orotate + 5-phospho-alpha-D-ribose 1-diphosphate
-
 Homo sapiens orotidine 5'-phosphate + diphosphate
-
 ?
2.4.2.10 orotate + 5-phospho-alpha-D-ribose 1-diphosphate
-
 Plasmodium falciparum orotidine 5'-phosphate + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.2.10 OPRT
-
 Homo sapiens
2.4.2.10 OPRT
-
 Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.2.10 0.00004
-
 4-nitrophenyl beta-D-ribose 5'-phosphate at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.000041
-
 4-nitrophenyl beta-D-ribose 5'-phosphate at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.00012
-
 4-nitrophenyl beta-D-ribose at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.00019
-
 4-nitrophenyl beta-D-ribose at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.08
-
 (2R,3R,4S)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.083
-
 (3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.09
-
 [(7R,8R,9S,9aS)-8,9-dihydroxy-1,3,5-trioxo-1,2,3,5,8,9,9a,10-octahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidin-7-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.11
-
 (7R,8R,9S,9aS)-8,9-dihydroxy-7-(hydroxymethyl)-8,9,9a,10-tetrahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidine-1,3,5(2H)-trione at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.12
-
 1,3-dihydroxy-N-[2-(4-nitrophenyl)ethyl]propan-2-aminium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.14
-
 [(2R,3R,4S,5S)-5-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.15
-
 1,3-dihydroxy-N-[(4-nitrophenyl)methyl]propan-2-aminium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.17
-
 [(7R,8R,9S,9aS)-8,9-dihydroxy-1,3,5-trioxo-1,2,3,5,8,9,9a,10-octahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidin-7-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.2
-
 [(2R,3R,4S,5S)-5-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.2
-
 (1R,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[(4-nitrophenyl)methyl]pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.22
-
 (3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.23
-
 (2R,3S)-3-hydroxy-2-(hydroxymethyl)-5-(4-nitrophenyl)pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.23
-
 (1S,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[2-(4-nitrophenyl)ethyl]pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.24
-
 [(3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-4-hydroxypyrrolidin-1-ium-3-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.25
-
 1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.27
-
 (7R,8R,9S,9aS)-8,9-dihydroxy-7-(hydroxymethyl)-8,9,9a,10-tetrahydro-7H-pyrrolo[1',2':4,5]pyrazino[1,2-c]pyrimidine-1,3,5(2H)-trione at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.27
-
 (2R,3R,4S)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.29
-
 (2R,3R,4S)-1-[2-(6-carboxy-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.3
-
 (2S,3S,4R,5R)-2-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.35
-
 (2S,3S,4R,5R)-2-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.35
-
 [(2R,3R,4S,5S)-5-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.36
-
 (2S,3S,4R,5R)-2-[(6-cyano-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.37
-
 [(2R,3R,4S,5S)-5-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.47
-
 1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.48
-
 (2R,3S)-3-hydroxy-2-(hydroxymethyl)-5-(4-nitrophenyl)pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.5
-
 [(3R,4R)-1-[(6-carboxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl]-4-hydroxypyrrolidin-1-ium-3-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.5
-
 1,3-dihydroxy-N-[(4-nitrophenyl)methyl]propan-2-aminium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.51
-
 1,3-dihydroxy-N-[2-(4-nitrophenyl)ethyl]propan-2-aminium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.52
-
 (3R,4R)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.53
-
 (2S,3S,4R,5R)-2-[(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Homo sapiens
2.4.2.10 0.57
-
 (1S,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[2-(4-nitrophenyl)ethyl]pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.69
-
 (2R,3R,4S)-1-[2-(6-carboxy-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3,4-dihydroxy-2-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 0.75
-
 (1R,3R,4R)-3-hydroxy-4-(hydroxymethyl)-1-[(4-nitrophenyl)methyl]pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 1.3
-
 (3R,4R)-1-[2-(5-bromo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethyl]-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-ium at pH 8.0 and 25°C Plasmodium falciparum
2.4.2.10 4.3
-
 [(2R,3R,4S,5S)-5-(4-carboxypyridin-3-yl)-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Homo sapiens
2.4.2.10 15.5
-
 [(2R,3R,4S,5S)-5-(4-carboxypyridin-3-yl)-3,4-dihydroxypyrrolidin-1-ium-2-yl]methyl hydrogen phosphate at pH 8.0 and 25°C Plasmodium falciparum