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Literature summary extracted from

  • Arrebola, R.; Olmo, A.; Reche, P.; Garvey, E.P.; Santi, D.V.; Ruiz-Perez, L.M.; Gonzalez-Pacanowska, D.
    Isolation and characterization of a mutant dihydrofolate reductase-thymidylate synthase from methotrexate-resistant Leishmania cells (1994), J. Biol. Chem., 269, 10590-10596.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.5.1.3 medicine drug target Leishmania major

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.5.1.3 cloning of gene encoding mutant R53M enzyme from methotrexate-resistant strain into an expression plasmid, expression in Escherichia coli Leishmania major

Protein Variants

EC Number Protein Variants Comment Organism
1.5.1.3 R53M resistance providing naturally occurring mutant from methotrexate-resistant strain, lower turnover number Leishmania major

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 methotrexate wild-type enzyme, slow binding Leishmania major
1.5.1.3 additional information binding study of mutant R53M enzyme from methotrexate resistant strain with methotrexate Leishmania major

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.5.1.3 0.0009
-
 NADPH wild-type enzyme Leishmania major
1.5.1.3 0.0012
-
 NADPH mutant R53M enzyme Leishmania major
1.5.1.3 0.0013
-
 7,8-dihydrofolate wild-type enzyme Leishmania major
1.5.1.3 0.0016
-
 7,8-dihydrofolate mutant R53M enzyme Leishmania major

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Leishmania major
-
 bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
1.5.1.3 Leishmania major
-
 methotrexate-resistant strain with altered enzyme
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.5.1.3 8
-
 wild-type enzyme Leishmania major
1.5.1.3 15
-
 mutant R53M enzyme Leishmania major

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH
-
 Leishmania major 5,6,7,8-tetrahydrofolate + NADP+
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.5.1.3 7.6
-
 7,8-dihydrofolate mutant R53M enzyme Leishmania major
1.5.1.3 29
-
 7,8-dihydrofolate wild-type enzyme Leishmania major

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADPH
-
 Leishmania major

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.3 0.000018
-
 methotrexate wild-type enzyme Leishmania major