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Literature summary for 2.5.1.58 extracted from

  • Coudray, L.; de Figueiredo, R.M.; Duez, S.; Cortial, S.; Dubois, J.
    Synthesis of imidazole-containing analogues of farnesyl pyrophosphate and evaluation of their biological activity on protein farnesyltransferase (2009), J. Enzyme Inhib. Med. Chem., 24, 972-985.
    View publication on PubMed
Search for more literature for 2.5.1.58

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli BL21 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
-
 Homo sapiens
(2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
-
 Saccharomyces cerevisiae
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
-
 Homo sapiens
(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
-
 Saccharomyces cerevisiae
(2Z)-3-(1H-imidazol-2-yl)-5-methylhexa-2,4-dienoic acid 8% inhibition at 0.001 M Saccharomyces cerevisiae
(2Z)-5-methyl-3-(1-methyl-1H-imidazol-2-yl)hexa-2,4-dienoic acid 8% inhibition at 0.001 M Saccharomyces cerevisiae
(2Z,4E)-5,9-dimethyl-3-(1-methyl-1H-imidazol-2-yl)deca-2,4,8-trienoic acid
-
 Homo sapiens
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
-
 Homo sapiens
(2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
-
 Saccharomyces cerevisiae
(4E)-5,9-dimethyl-3-(1-methyl-1H-imidazol-2-yl)deca-4,8-dienoic acid
-
 Homo sapiens
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
-
 Homo sapiens
(4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
-
 Saccharomyces cerevisiae
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
-
 Homo sapiens
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
-
 Saccharomyces cerevisiae
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
-
 Homo sapiens
2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
-
 Saccharomyces cerevisiae
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
-
 Homo sapiens
2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
-
 Saccharomyces cerevisiae
3-(1H-imidazol-2-yl)-5-methylhex-4-enoic acid 21% inhibition at 0.001 M Saccharomyces cerevisiae
5-methyl-3-(1-methyl-1H-imidazol-2-yl)hex-4-enoic acid 25% inhibition at 0.001 M Saccharomyces cerevisiae
chaetomellic acid A
-
 Homo sapiens
chaetomellic acid A
-
 Saccharomyces cerevisiae
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
-
 Homo sapiens
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate 50% growth inhibition at 0.03 mM Plasmodium falciparum
di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
-
 Saccharomyces cerevisiae
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
-
 Homo sapiens
tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
-
 Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-
Saccharomyces cerevisiae
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens
-
 Saccharomyces cerevisiae
-
 Plasmodium falciparum

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
-
 ?
(2E,6E)-farnesyl diphosphate + [protein]-L-cysteine assay at pH 7.5, 30°C Homo sapiens [protein]-S-((2E,6E)-farnesyl)-L-cysteine + diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
FTase
-
 Homo sapiens
FTase
-
 Saccharomyces cerevisiae
FTase
-
 Plasmodium falciparum
protein farnesyltransferase
-
 Homo sapiens
protein farnesyltransferase
-
 Saccharomyces cerevisiae
protein farnesyltransferase
-
 Plasmodium falciparum

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000175
-
 30°C, pH 7.5 Homo sapiens chaetomellic acid A
0.00034
-
 30°C, pH 7.5 Saccharomyces cerevisiae chaetomellic acid A
0.0025
-
 30°C, pH 7.5 Saccharomyces cerevisiae 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
0.0054
-
 30°C, pH 7.5 Homo sapiens 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]butanedioic acid
0.0065
-
 30°C, pH 7.5 Homo sapiens (2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
0.012
-
 30°C, pH 7.5 Homo sapiens (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
0.016
-
 30°C, pH 7.5 Saccharomyces cerevisiae (2E)-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]butanedioic acid
0.028
-
 30°C, pH 7.5 Saccharomyces cerevisiae (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
0.04
-
 30°C, pH 7.5 Saccharomyces cerevisiae (2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
0.042
-
 30°C, pH 7.5 Saccharomyces cerevisiae (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
0.13
-
 30°C, pH 7.5 Homo sapiens (2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
0.13
-
 30°C, pH 7.5 Saccharomyces cerevisiae (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
0.17
-
 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
0.175
-
 30°C, pH 7.5 Homo sapiens (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoic acid
0.3
-
 30°C, pH 7.5 Homo sapiens tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
0.5
-
 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
0.59
-
 30°C, pH 7.5 Homo sapiens 2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid
0.6
-
 30°C, pH 7.5 Saccharomyces cerevisiae tert-butyl (2Z,4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-2,4,8,12-tetraenoate
0.7
-
 30°C, pH 7.5 Saccharomyces cerevisiae (4E,8E)-5,9,13-trimethyl-3-(1-methyl-1H-imidazol-2-yl)tetradeca-4,8,12-trienoic acid
0.7
-
 30°C, pH 7.5 Homo sapiens di-tert-butyl 2-[(2E,6E,10E)-1,3,7-trimethyl-1-(1-methyl-1H-imidazol-2-yl)dodeca-2,6,10-trien-1-yl]butanedioate
0.85
-
 30°C, pH 7.5 Saccharomyces cerevisiae 2-[(2E)-3,7-dimethyl-1-(1-methyl-1H-imidazol-2-yl)octa-2,6-dien-1-yl]butanedioic acid