Literature summary for 2.1.2.2 extracted from

Zhang, Y.; Desharnais, J.; Marsilje, T.H.; Li, C.; Hedrick, M.P.; Gooljarsingh, L.T.; Tavassoli, A.; Benkovic, S.J.; Olson, A.J.; Boger, D.L.; Wilson, I.A.
Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid (2003), Biochemistry, 42, 6043-6056.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
vapor diffusion sitting drop method, crystals of enzyme in complex with 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid	specifically inhibits recombinant GAR Tfase, inactive against other folate-dependent enzymes, potent inhibitor of tumor cell proliferation	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P22102	-	-

Synonyms

Synonyms	Comment	Organism
GAR TFase	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000015	-	10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid	-	Homo sapiens

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Release 2023.1 (January 2023)