Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Paiardini, A.; Fiascarelli, A.; Rinaldo, S.; Daidone, F.; Giardina, G.; Koes, D.R.; Parroni, A.; Montini, G.; Marani, M.; Paone, A.; McDermott, L.A.; Contestabile, R.; Cutruzzola, F.
    Screening and in vitro testing of antifolate inhibitors of human cytosolic serine hydroxymethyltransferase (2015), ChemMedChem, 10, 490-497 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.2.1 lometrexol competitive inhibition Homo sapiens
2.1.2.1 methotrexate
-
 Homo sapiens
2.1.2.1 nolatrexed poor inhibition Homo sapiens
2.1.2.1 pemetrexed i.e. (S)-2-[4-[2-(4-amino-2-oxo-3,5,7-triazabicyclo[4.3.0]nona-3,8,10-trien-9-yl) ethyl] benzoyl]aminopentanedioic acid, brand name Alimta, low micromolar inhibitor Homo sapiens
2.1.2.1 raltitrexed
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.1.2.1 cytosol
-
 Homo sapiens 5829
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.2.1 5,10-methylenetetrahydrofolate + glycine + H2O Homo sapiens
-
 tetrahydrofolate + L-serine
-
 r
2.1.2.1 tetrahydrofolate + L-serine Homo sapiens
-
 5,10-methylenetetrahydrofolate + glycine + H2O
-
 r

Organism

EC Number Organism UniProt Comment Textmining
2.1.2.1 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.2.1
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.2.1 5,10-methylenetetrahydrofolate + glycine + H2O
-
 Homo sapiens tetrahydrofolate + L-serine
-
 r
2.1.2.1 tetrahydrofolate + L-serine
-
 Homo sapiens 5,10-methylenetetrahydrofolate + glycine + H2O
-
 r

Synonyms

EC Number Synonyms Comment Organism
2.1.2.1 serine hydroxymethyltransferase
-
 Homo sapiens
2.1.2.1 SHMT1
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.1.2.1 pyridoxal 5'-phosphate
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.2.1 0.023
-
 lometrexol at pH 7.2 and 30°C Homo sapiens
2.1.2.1 0.122
-
 raltitrexed at pH 7.2 and 30°C Homo sapiens
2.1.2.1 0.201
-
 methotrexate at pH 7.2 and 30°C Homo sapiens
2.1.2.1 1
-
 nolatrexed Ki above 1 mM, at pH 7.2 and 30°C Homo sapiens