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Literature summary for 2.5.1.58 extracted from

  • Pinel, B.; Dubois, J.; Seraphin, D.; Richomme, P.
    Semisynthesis of alpha-methyl-gamma-lactones and in vitro evaluation of their activity on protein farnesyltransferase (2010), J. Enzyme Inhib. Med. Chem., 25, 172-179.
    View publication on PubMed
Search for more literature for 2.5.1.58

Inhibitors

Inhibitors Comment Organism Structure
(1aR,2S,3aS,6aR,7aR)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
 Saccharomyces cerevisiae
(1aR,2S,3aS,6aR,7aR)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
 Saccharomyces cerevisiae
(1aS,2S,3aS,6aR,7aS)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
 Saccharomyces cerevisiae
(1aS,2S,3aS,6aR,7aS)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
-
 Saccharomyces cerevisiae
(2E)-3-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-1-methylprop-2-en-1-yl acetate
-
 Saccharomyces cerevisiae
(3aR,7S,8aS)-3,7-dimethyl-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
 Saccharomyces cerevisiae
(3aR,7S,8aS)-6-[(1E)-3-hydroxybut-1-en-1-yl]-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
 Saccharomyces cerevisiae
(3aR,7S,8aS)-7-methyl-3-methylidene-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
 Saccharomyces cerevisiae
(3aR,8S,9aS)-6-acetyl-3,8-dimethyl-3,3a,4,8,9,9a-hexahydro-2H-cyclohepta[1,2-b:4,5-b']difuran-2-one
-
 Saccharomyces cerevisiae
(3R,3aR,7S,8aS)-3,7-dimethyl-6-(3-oxobutyl)-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
 Saccharomyces cerevisiae
(3R,3aR,7S,8aS)-6-(3-hydroxybutyl)-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
-
 Saccharomyces cerevisiae
1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-(1-hydroxyethoxy)butyl acetate
-
 Saccharomyces cerevisiae
1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
-
 Saccharomyces cerevisiae
1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-oxobutyl acetate
-
 Saccharomyces cerevisiae
1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
-
 Saccharomyces cerevisiae
3-hydroxy-1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butyl acetate
-
 Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Saccharomyces cerevisiae
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Saccharomyces cerevisiae

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(2E,6E)-farnesyl diphosphate + dansyl-GCVLS assay at pH 7.5, 30°C Saccharomyces cerevisiae dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
PFTase
-
 Saccharomyces cerevisiae
protein farnesyltransferase
-
 Saccharomyces cerevisiae

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Saccharomyces cerevisiae

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Saccharomyces cerevisiae

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.04
-
 30°C, pH 7.5 Saccharomyces cerevisiae 1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
0.04
-
 30°C, pH 7.5 Saccharomyces cerevisiae 1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butane-1,3-diyl diacetate
0.066
-
 30°C, pH 7.5 Saccharomyces cerevisiae (1aS,2S,3aS,6aR,7aS)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
0.09
-
 30°C, pH 7.5 Saccharomyces cerevisiae (1aR,2S,3aS,6aR,7aR)-2,6-dimethyl-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
0.1
-
 30°C, pH 7.5 Saccharomyces cerevisiae (1aR,2S,3aS,6aR,7aR)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
0.1
-
 30°C, pH 7.5 Saccharomyces cerevisiae (3aR,7S,8aS)-7-methyl-3-methylidene-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
0.15
-
 30°C, pH 7.5 Saccharomyces cerevisiae 1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-oxobutyl acetate
0.21
-
 30°C, pH 7.5 Saccharomyces cerevisiae (3aR,7S,8aS)-3,7-dimethyl-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
0.24
-
 30°C, pH 7.5 Saccharomyces cerevisiae (3R,3aR,7S,8aS)-3,7-dimethyl-6-(3-oxobutyl)-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
0.5
-
 30°C, pH 7.5 Saccharomyces cerevisiae (1aS,2S,3aS,6aR,7aS)-2-methyl-6-methylidene-1a-[(1E)-3-oxobut-1-en-1-yl]octahydro-5H-oxireno[4,5]cyclohepta[1,2-b]furan-5-one
0.633
-
 30°C, pH 7.5 Saccharomyces cerevisiae 1-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-3-(1-hydroxyethoxy)butyl acetate
0.9
-
 30°C, pH 7.5 Saccharomyces cerevisiae (2E)-3-[(3aR,7S,8aS)-3,7-dimethyl-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]-1-methylprop-2-en-1-yl acetate
1
-
 value above, 30°C, pH 7.5 Saccharomyces cerevisiae (3aR,7S,8aS)-6-[(1E)-3-hydroxybut-1-en-1-yl]-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
1
-
 value above, 30°C, pH 7.5 Saccharomyces cerevisiae (3R,3aR,7S,8aS)-6-(3-hydroxybutyl)-3,7-dimethyl-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
1
-
 value above, 30°C, pH 7.5 Saccharomyces cerevisiae 3-hydroxy-1-[(3aR,7S,8aS)-7-methyl-3-methylidene-2-oxo-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-6-yl]butyl acetate
1
-
 value above, 330°C, pH 7.5 Saccharomyces cerevisiae (3aR,8S,9aS)-6-acetyl-3,8-dimethyl-3,3a,4,8,9,9a-hexahydro-2H-cyclohepta[1,2-b:4,5-b']difuran-2-one