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Literature summary extracted from

  • Hekmat-Nejad, M.; Rathod, P.K.
    Kinetics of Plasmodium flaciparum thymidylate synthase: interactions with high-affinity metabolites of 5-fluoroorotate and D1694 (1996), Antimicrob. Agents Chemother., 40, 1628-1632.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.1.1.45 medicine
-
 Mus musculus
2.1.1.45 medicine
-
 Homo sapiens
2.1.1.45 medicine
-
 Crithidia fasciculata
2.1.1.45 medicine
-
 Plasmodium berghei
2.1.1.45 medicine development of antimalarial drugs, selective chemoptherapy directed at malarial TS, inhibitors of pyrimidine biosynthesis shall be considered for malaria chemotherapy Plasmodium falciparum

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.1.1.45 Escherichia coli cells carrying an expression plasmid with the malarial dihydrofolate reductase-thymidylate synthase Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Escherichia coli
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Leishmania major
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Mus musculus
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Plasmodium falciparum
2.1.1.45 5-Fluoroorotate
-
 Plasmodium falciparum
2.1.1.45 5-Fluoroorotate
-
 Plasmodium yoelii
2.1.1.45 5-fluorouracil
-
 Crithidia fasciculata
2.1.1.45 5-fluorouracil
-
 Escherichia coli
2.1.1.45 5-fluorouracil
-
 Homo sapiens
2.1.1.45 5-fluorouracil
-
 Plasmodium falciparum
2.1.1.45 D1694
-
 Mus musculus
2.1.1.45 D1694
-
 Plasmodium falciparum
2.1.1.45 D1694 pentaglutamate
-
 Mus musculus
2.1.1.45 D1694 pentaglutamate
-
 Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.1.1.45 0.0013
-
 2'-deoxyuridylate native enzyme Plasmodium falciparum
2.1.1.45 0.0018
-
 2'-deoxyuridylate
-
 Homo sapiens
2.1.1.45 0.002
-
 2'-deoxyuridylate recombinant enzyme Plasmodium falciparum
2.1.1.45 0.0034
-
 2'-deoxyuridylate
-
 Escherichia coli
2.1.1.45 0.008
-
 methylenetetrahydrofolate
-
 Homo sapiens
2.1.1.45 0.027
-
 methylenetetrahydrofolate
-
 Mus musculus
2.1.1.45 0.03
-
 5,10-methylenetetrahydrofolate native enzyme Plasmodium falciparum
2.1.1.45 0.031
-
 methylenetetrahydrofolate
-
 Homo sapiens
2.1.1.45 0.039
-
 5,10-methylenetetrahydrofolate recombinant enzyme Plasmodium falciparum

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.1.1.45 31000
-
 2 * 31000, SDS-PAGE Escherichia coli
2.1.1.45 31000
-
 2 * 31000, SDS-PAGE Plasmodium falciparum
2.1.1.45 71000
-
-
 Mus musculus
2.1.1.45 71000
-
-
 Plasmodium falciparum

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Mus musculus
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Escherichia coli
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Homo sapiens
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Crithidia fasciculata
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Plasmodium falciparum
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Plasmodium berghei
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Leishmania major
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Plasmodium yoelii
-
 dihydrofolate + dTMP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.45 Crithidia fasciculata
-
-
-
2.1.1.45 Escherichia coli
-
-
-
2.1.1.45 Homo sapiens
-
-
-
2.1.1.45 Leishmania major
-
 formerly called Leishmania tropica
-
2.1.1.45 Mus musculus
-
-
-
2.1.1.45 Plasmodium berghei
-
-
-
2.1.1.45 Plasmodium falciparum
-
-
-
2.1.1.45 Plasmodium yoelii
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.1.45 recombinant enzyme, expressed in E. coli Plasmodium falciparum

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.1.1.45 0.0255
-
-
 Plasmodium falciparum

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.45 5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
-
 Homo sapiens 7,8-dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Mus musculus dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Mus musculus dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Escherichia coli dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Escherichia coli dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Homo sapiens dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Homo sapiens dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Crithidia fasciculata dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Crithidia fasciculata dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Plasmodium falciparum dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Plasmodium falciparum dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Plasmodium berghei dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Plasmodium berghei dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Leishmania major dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Leishmania major dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Plasmodium yoelii dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Plasmodium yoelii dihydrofolate + dTMP
-
 r
2.1.1.45 additional information
-
 Escherichia coli ?
-
 ?
2.1.1.45 additional information
-
 Homo sapiens ?
-
 ?
2.1.1.45 additional information bifunctional enzyme dihydrofolate reductase-thymidylate synthase Plasmodium falciparum ?
-
 ?
2.1.1.45 additional information bifunctional enzyme dihydrofolate reductase-thymidylate synthase Leishmania major ?
-
 ?
2.1.1.45 [6R,S]-5,10-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
-
 Mus musculus ?
-
 ?

Subunits

EC Number Subunits Comment Organism
2.1.1.45 dimer
-
 Mus musculus
2.1.1.45 dimer
-
 Homo sapiens
2.1.1.45 dimer
-
 Plasmodium berghei
2.1.1.45 dimer
-
 Leishmania major
2.1.1.45 dimer 2 * 31000, SDS-PAGE Escherichia coli
2.1.1.45 dimer 2 * 31000, SDS-PAGE Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.45 0.00000006
-
 D1694
-
 Mus musculus
2.1.1.45 0.000001
-
 D1694 pentaglutamate
-
 Mus musculus
2.1.1.45 0.0000015
-
 D1694 pentaglutamate
-
 Plasmodium falciparum
2.1.1.45 0.0000017
-
 5-fluoro-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 0.000002
-
 5-fluoro-2'-deoxyuridylic acid
-
 Plasmodium falciparum
2.1.1.45 0.0000028
-
 D1694
-
 Plasmodium falciparum
2.1.1.45 0.002
-
 5-fluoro-2'-deoxyuridylic acid
-
 Plasmodium falciparum