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Literature summary for 2.1.2.1 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
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Inhibitors

Inhibitors Comment Organism Structure
lometrexol competitive inhibition Homo sapiens
methotrexate
-
 Homo sapiens
nolatrexed poor inhibition Homo sapiens
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
raltitrexed
-
 Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
serine hydroxymethyltransferase
-
 Homo sapiens
SHMT1
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
pyridoxal 5'-phosphate
-
 Homo sapiens

Ki Value [mM]

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