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Literature summary for 2.5.1.58 extracted from

  • de Figueiredo, R.M.; Coudray, L.; Dubois, J.
    Synthesis and biological evaluation of potential bisubstrate inhibitors of protein farnesyltransferase. Design and synthesis of functionalized imidazoles (2007), Org. Biomol. Chem., 5, 3299-3309.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Saccharomyces cerevisiae

Inhibitors

Inhibitors Comment Organism Structure
BMS-214662 the commercial name is Zamestra Saccharomyces cerevisiae
methyl N-([2-[4-ethoxy-2-(ethoxycarbonyl)-4-oxobutyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
Saccharomyces cerevisiae
methyl N-([2-[4-ethoxy-2-(ethoxycarbonyl)-4-oxobutyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-Lisoleucyl-L-alaninate
-
Saccharomyces cerevisiae
methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate
-
Saccharomyces cerevisiae
methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
Saccharomyces cerevisiae
methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate
-
Saccharomyces cerevisiae
methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
Saccharomyces cerevisiae
N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
-
Saccharomyces cerevisiae
N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
-
Saccharomyces cerevisiae
N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
-
Saccharomyces cerevisiae
N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
-
Saccharomyces cerevisiae
N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
-
Saccharomyces cerevisiae
N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-Lisoleucyl-L-alanine
-
Saccharomyces cerevisiae
tipifarnib
-
Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Saccharomyces cerevisiae
-
-
-

Purification (Commentary)

Purification (Comment) Organism
partially purified Saccharomyces cerevisiae

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + dansyl-GCVLS
-
Saccharomyces cerevisiae diphosphate + S-farnesyl dansyl-GCVLS
-
?

Synonyms

Synonyms Comment Organism
FTase
-
Saccharomyces cerevisiae

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.035
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
0.08
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
0.08
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
0.15
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
0.18
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae N-[[2-(4,5-dicarboxypentyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-Lisoleucyl-L-alanine
0.19
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
0.27
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae N-[[2-(2,3-dicarboxypropyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-isoleucyl-L-alanine
0.34
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae methyl N-([2-[6-ethoxy-4-(ethoxycarbonyl)-6-oxohexyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate
0.4
-
in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae N-[[2-(3,4-dicarboxybutyl)-1-methyl-1H-imidazol-5-yl]methyl]-L-valyl-L-phenylalanyl-L-methionine
1
-
IC50 above 1 mM, in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae methyl N-([2-[4-ethoxy-2-(ethoxycarbonyl)-4-oxobutyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
1
-
IC50 above 1 mM, in 5.8 mM dithiothreitol, 12 mM MgCl2, 0.012 mM ZnCl2 and 0.09% (w/v) CHAPS, 53 mM Tris-HCl, at pH 7.5 and 30°C Saccharomyces cerevisiae methyl N-([2-[5-ethoxy-3-(methoxycarbonyl)-5-oxopentyl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-isoleucyl-L-alaninate