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Literature summary for 2.1.2.1 extracted from

  • Scaletti, E.; Jemth, A.S.; Helleday, T.; Stenmark, P.
    Structural basis of inhibition of the human serine hydroxymethyltransferase SHMT2 by antifolate drugs (2019), FEBS Lett., 593, 1863-1873 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3)-TIR cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting drop vapor diffusion method, using 0.1 M Bis-Tris pH 6.5, 28% (w/v) PEGMME 2000 (in complex with lometrexol and methotrexate), 0.2 M LiCl2, 0.1 M MES pH 6.0, 20% (w/v) PEG6000 (in complex with pemetrexed), and 0.2 M NaCl, 0.1 M MES pH 6.0, 20% (w/v) PEG6000 (in complex with raltitrexed) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
lometrexol 49.7% residual activity at 0.1 mM Homo sapiens
methotrexate 87.4% residual activity at 0.1 mM Homo sapiens
pemetrexed 79.2% residual activity at 0.1 mM Homo sapiens
raltitrexed 94% residual activity at 0.1 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
Homo sapiens 5739
-

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 P34897
-
-

Purification (Commentary)

Purification (Comment) Organism
His-Trap column chromatography and Superdex 75 gel filtration 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

Subunits

Subunits Comment Organism
tetramer
-
Homo sapiens

Synonyms

Synonyms Comment Organism
serine hydroxymethyltransferase
-
Homo sapiens
SHMT2
-
Homo sapiens

Cofactor

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