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Literature summary for 2.5.1.58 extracted from

  • Long, C.; Marcourt, L.; Raux, R.; David, B.; Gau, C.; Menendez, C.; Gao, M.; Laroche, M.F.; Schambel, P.; Delaude, C.; Ausseil, F.; Lavaud, C.; Massiot, G.
    Meroterpenes from Dichrostachys cinerea inhibit protein farnesyl transferase activity (2009), J. Nat. Prod., 72, 1804-1815.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carbaldehyde
-
Rattus norvegicus
(1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carboxylic acid
-
Rattus norvegicus
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-5-[[(1S,3S,7S,8aS)-1,3,7-trihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
Rattus norvegicus
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
Rattus norvegicus
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,5R,8aS)-3-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
Rattus norvegicus
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,7S,8aS)-3,7-dihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
Rattus norvegicus
(4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
Rattus norvegicus
(4aS,5R,8aR)-4a-(5-hydroxy-7-methoxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
Rattus norvegicus
(4aS,5S,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,2R,7S,8aS)-2,7-dihydroxy-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl]methyl]-6-hydroxy-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
-
Rattus norvegicus
1,4,8,10-tetrahydroxy-6-[(1E)-3-[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]-1-methylprop-1-en-1-yl]-5,6-dihydro-7H-benzo[c]xanthen-7-one
-
Rattus norvegicus
5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-6-methyl-4-oxo-1,5,8,8a-tetrahydronaphthalen-4a(4H)-yl]-4H-chromen-4-one
-
Rattus norvegicus
5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-6-methyl-2-oxo-1,5,8,8a-tetrahydronaphthalen-4a(2H)-yl]-4H-chromen-4-one
-
Rattus norvegicus
SCH-66336
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(2E,6E)-farnesyl diphosphate + dansyl-CGVLS assay at pH 7.5, 37°C Rattus norvegicus dansyl-G-(S-(2E,6E)-farnesyl)CVLS
-
?

Synonyms

Synonyms Comment Organism
protein farnesyl transferase
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
30°C, pH 7.5 Rattus norvegicus SCH-66336
0.0018
-
30°C, pH 7.5 Rattus norvegicus (1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carbaldehyde
0.003
-
30°C, pH 7.5 Rattus norvegicus (4aS,5R,8aR)-4a-(5-hydroxy-7-methoxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
0.0032
-
30°C, pH 7.5 Rattus norvegicus (4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-6-methyl-5-[[(1R,8aS)-5,5,8a-trimethyl-2-methylidene-3-oxodecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
0.0057
-
30°C, pH 7.5 Rattus norvegicus (4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
0.007
-
30°C, pH 7.5 Rattus norvegicus 5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-6-methyl-2-oxo-1,5,8,8a-tetrahydronaphthalen-4a(2H)-yl]-4H-chromen-4-one
0.01
-
30°C, pH 7.5 Rattus norvegicus (4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,5R,8aS)-3-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
0.017
-
30°C, pH 7.5 Rattus norvegicus (4aS,5S,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,2R,7S,8aS)-2,7-dihydroxy-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl]methyl]-6-hydroxy-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
0.025
-
30°C, pH 7.5 Rattus norvegicus 5,7-dihydroxy-2-[(5R)-1-hydroxy-5-[[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-6-methyl-4-oxo-1,5,8,8a-tetrahydronaphthalen-4a(4H)-yl]-4H-chromen-4-one
0.037
-
30°C, pH 7.5 Rattus norvegicus 1,4,8,10-tetrahydroxy-6-[(1E)-3-[(3S,8aS)-3-hydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]-1-methylprop-1-en-1-yl]-5,6-dihydro-7H-benzo[c]xanthen-7-one
0.04
-
30°C, pH 7.5 Rattus norvegicus (1R,4aR,5R,7S)-5-[[(1R,4aR,8aS)-8a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-6-methoxy-5,8-dioxo-1,4,4a,5,8,8a-hexahydronaphthalen-1-yl]methyl]-7-hydroxy-1,4a-dimethyl-6-methylidenedecahydronaphthalene-1-carboxylic acid
0.04
-
30°C, pH 7.5 Rattus norvegicus (4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-5-[[(1R,3S,7S,8aS)-3,7-dihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-2-methoxy-4a,5,8,8a-tetrahydronaphthalene-1,4-dione
0.086
-
30°C, pH 7.5 Rattus norvegicus (4aS,5R,8aR)-4a-(5,7-dihydroxy-4-oxo-4H-chromen-2-yl)-2-methoxy-5-[[(1S,3S,7S,8aS)-1,3,7-trihydroxy-5,5,8a-trimethyl-2-methylidenedecahydronaphthalen-1-yl]methyl]-4a,5,8,8a-tetrahydronaphthalene-1,4-dione