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

BRENDA support

Literature summary for 2.5.1.58 extracted from

  • Ohkanda, J.; Strickland, C.L.; Blaskovich, M.A.; Carrico, D.; Lockman, J.W.; Vogt, A.; Bucher, C.J.; Sun, J.; Qian, Y.; Knowles, D.; Pusateri, E.E.; Sebti, S.M.; Hamilton, A.D.
    Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase (2006), Org. Biomol. Chem., 4, 482-492.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-[N, N -bis((1H-imidazol-4-yl)methyl)aminomethyl]-2-(1-(o-tolyl))benzoylmethionine trifluoroacetate IC50: 1.7 nM Mus musculus
4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methoxyphenyl)-benzoylmethionine IC50: 9.5 nM Mus musculus
4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methylphenyl)-benzoylmethionine IC50: 2.8 nM Mus musculus
4-[N-(1H-imidazol-4-yl)methylamino]-2-phenylbenzoylmethionine IC50: 28 nM Mus musculus
FTI-2148 IC50: 0.86 nM Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + protein-cysteine
-
Mus musculus diphosphate + S-farnesyl protein
-
?

Synonyms

Synonyms Comment Organism
PFTase
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000086
-
IC50: 0.86 nM Mus musculus FTI-2148
0.0000017
-
IC50: 1.7 nM Mus musculus 4-[N, N -bis((1H-imidazol-4-yl)methyl)aminomethyl]-2-(1-(o-tolyl))benzoylmethionine trifluoroacetate
0.0000028
-
IC50: 2.8 nM Mus musculus 4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methylphenyl)-benzoylmethionine
0.0000095
-
IC50: 9.5 nM Mus musculus 4-[N-(1-H-imidazol-4-yl)methylamino]-2-(2-methoxyphenyl)-benzoylmethionine
0.000028
-
IC50: 28 nM Mus musculus 4-[N-(1H-imidazol-4-yl)methylamino]-2-phenylbenzoylmethionine