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Literature summary extracted from

  • Duez, S.; Coudray, L.; Mouray, E.; Grellier, P.; Dubois, J.
    Towards the synthesis of bisubstrate inhibitors of protein farnesyltransferase: Synthesis and biological evaluation of new farnesylpyrophosphate analogues (2010), Bioorg. Med. Chem., 18, 543-556.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.58 (2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
-
 Homo sapiens
2.5.1.58 (2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
-
 Saccharomyces cerevisiae
2.5.1.58 (4E,8E)-2-(ethoxycarbonyl)-5,9,13-trimethyl-2-[3-(1-methyl-1H-imidazol-2-yl)propyl]tetradeca-4,8,12-trienoic acid
-
 Homo sapiens
2.5.1.58 (4E,8E)-2-(ethoxycarbonyl)-5,9,13-trimethyl-2-[3-(1-methyl-1H-imidazol-2-yl)propyl]tetradeca-4,8,12-trienoic acid 50% growth inhibition at 0.004 mM Plasmodium falciparum
2.5.1.58 (4E,8E)-2-(ethoxycarbonyl)-5,9,13-trimethyl-2-[3-(1-methyl-1H-imidazol-2-yl)propyl]tetradeca-4,8,12-trienoic acid
-
 Trypanosoma brucei
2.5.1.58 (4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
-
 Homo sapiens
2.5.1.58 (4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
-
 Saccharomyces cerevisiae
2.5.1.58 (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienamide
-
 Homo sapiens
2.5.1.58 (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
-
 Homo sapiens
2.5.1.58 (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
-
 Saccharomyces cerevisiae
2.5.1.58 (4E,8E)-N-hydroxy-5,9,13-trimethyltetradeca-4,8,12-trienamide
-
 Homo sapiens
2.5.1.58 (6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
-
 Homo sapiens
2.5.1.58 (6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
-
 Saccharomyces cerevisiae
2.5.1.58 (7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
-
 Homo sapiens
2.5.1.58 (7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
-
 Saccharomyces cerevisiae
2.5.1.58 3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
-
 Homo sapiens
2.5.1.58 3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
-
 Saccharomyces cerevisiae
2.5.1.58 4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
-
 Homo sapiens
2.5.1.58 4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
-
 Saccharomyces cerevisiae
2.5.1.58 5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
-
 Homo sapiens
2.5.1.58 5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
-
 Saccharomyces cerevisiae
2.5.1.58 chaetomellic acid A
-
 Homo sapiens
2.5.1.58 chaetomellic acid A
-
 Saccharomyces cerevisiae
2.5.1.58 methyl N-([2-[(1E,6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate 50% growth inhibition at 0.0011 mM Plasmodium falciparum
2.5.1.58 methyl N-([2-[(1E,6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
 Trypanosoma brucei
2.5.1.58 methyl N-([2-[(6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate 50% growth inhibition at 0.001 mM Plasmodium falciparum
2.5.1.58 methyl N-([2-[(6E,10E)-4,4-bis(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methioninate
-
 Trypanosoma brucei
2.5.1.58 N-([2-[(1E,6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
-
 Homo sapiens
2.5.1.58 N-([2-[(1E,6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine 50% growth inhibition at 0.0172 mM Plasmodium falciparum
2.5.1.58 N-([2-[(6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
-
 Homo sapiens
2.5.1.58 N-([2-[(6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine 50% growth inhibition at 0.0314 mM Plasmodium falciparum
2.5.1.58 [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
-
 Homo sapiens
2.5.1.58 [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
-
 Saccharomyces cerevisiae
2.5.1.58 [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Homo sapiens
2.5.1.58 [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Saccharomyces cerevisiae
2.5.1.58 [(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
-
 Homo sapiens
2.5.1.58 [(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
-
 Saccharomyces cerevisiae
2.5.1.58 [3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Homo sapiens
2.5.1.58 [3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Plasmodium falciparum
2.5.1.58 [3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Trypanosoma brucei
2.5.1.58 [[(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoyl]amino]propanedioic acid
-
 Saccharomyces cerevisiae
2.5.1.58 [[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
-
 Homo sapiens
2.5.1.58 [[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
-
 Saccharomyces cerevisiae
2.5.1.58 [[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
-
 Homo sapiens
2.5.1.58 [[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
-
 Saccharomyces cerevisiae

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.58 Homo sapiens
-
-
-
2.5.1.58 Plasmodium falciparum
-
-
-
2.5.1.58 Saccharomyces cerevisiae
-
-
-
2.5.1.58 Trypanosoma brucei
-
-
-

Synonyms

EC Number Synonyms Comment Organism
2.5.1.58 FTase
-
 Homo sapiens
2.5.1.58 FTase
-
 Saccharomyces cerevisiae
2.5.1.58 FTase
-
 Trypanosoma brucei
2.5.1.58 FTase
-
 Plasmodium falciparum
2.5.1.58 protein farnesyltransferase
-
 Homo sapiens
2.5.1.58 protein farnesyltransferase
-
 Saccharomyces cerevisiae
2.5.1.58 protein farnesyltransferase
-
 Trypanosoma brucei
2.5.1.58 protein farnesyltransferase
-
 Plasmodium falciparum

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.5.1.58 30
-
 assay at Homo sapiens
2.5.1.58 30
-
 assay at Saccharomyces cerevisiae
2.5.1.58 30
-
 assay at Trypanosoma brucei
2.5.1.58 30
-
 assay at Plasmodium falciparum

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.5.1.58 7.5
-
 assay at Homo sapiens
2.5.1.58 7.5
-
 assay at Saccharomyces cerevisiae
2.5.1.58 7.5
-
 assay at Trypanosoma brucei
2.5.1.58 7.5
-
 assay at Plasmodium falciparum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.58 0.000175
-
 30°C, pH 7.5 Homo sapiens chaetomellic acid A
2.5.1.58 0.00024
-
 30°C, pH 7.5 Homo sapiens N-([2-[(6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-6,10,14-trien-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
2.5.1.58 0.00034
-
 30°C, pH 7.5 Saccharomyces cerevisiae chaetomellic acid A
2.5.1.58 0.00064
-
 30°C, pH 7.5 Homo sapiens N-([2-[(1E,6E,10E)-4-carboxy-4-(ethoxycarbonyl)-7,11,15-trimethylhexadeca-1,6,10,14-tetraen-1-yl]-1-methyl-1H-imidazol-5-yl]methyl)-L-valyl-L-phenylalanyl-L-methionine
2.5.1.58 0.00088
-
 30°C, pH 7.5 Homo sapiens [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
2.5.1.58 0.0009
-
 30°C, pH 7.5 Homo sapiens [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
2.5.1.58 0.004
-
 30°C, pH 7.5 Saccharomyces cerevisiae [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
2.5.1.58 0.005
-
 30°C, pH 7.5 Saccharomyces cerevisiae [[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
2.5.1.58 0.01
-
 30°C, pH 7.5 Homo sapiens [[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
2.5.1.58 0.015
-
 30°C, pH 7.5 Saccharomyces cerevisiae (7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
2.5.1.58 0.021
-
 30°C, pH 7.5 Homo sapiens [3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
2.5.1.58 0.035
-
 30°C, pH 7.5 Saccharomyces cerevisiae 5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
2.5.1.58 0.04
-
 30°C, pH 7.5 Saccharomyces cerevisiae (2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
2.5.1.58 0.042
-
 30°C, pH 7.5 Saccharomyces cerevisiae (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
2.5.1.58 0.06
-
 30°C, pH 7.5 Homo sapiens (7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
2.5.1.58 0.06
-
 30°C, pH 7.5 Homo sapiens 5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
2.5.1.58 0.06
-
 30°C, pH 7.5 Homo sapiens [[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
2.5.1.58 0.08
-
 30°C, pH 7.5 Saccharomyces cerevisiae (6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
2.5.1.58 0.08
-
 30°C, pH 7.5 Saccharomyces cerevisiae 3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
2.5.1.58 0.085
-
 30°C, pH 7.5 Homo sapiens [(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
2.5.1.58 0.1
-
 30°C, pH 7.5 Saccharomyces cerevisiae 4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
2.5.1.58 0.13
-
 30°C, pH 7.5 Homo sapiens (2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoic acid
2.5.1.58 0.13
-
 30°C, pH 7.5 Homo sapiens 4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
2.5.1.58 0.16
-
 30°C, pH 7.5 Homo sapiens 3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
2.5.1.58 0.17
-
 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
2.5.1.58 0.2
-
 30°C, pH 7.5 Saccharomyces cerevisiae (4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
2.5.1.58 0.2
-
 30°C, pH 7.5 Homo sapiens (6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
2.5.1.58 0.2
-
 30°C, pH 7.5 Saccharomyces cerevisiae [(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
2.5.1.58 0.2
-
 30°C, pH 7.5 Saccharomyces cerevisiae [[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
2.5.1.58 0.2
-
 value above, 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
2.5.1.58 0.2
-
 value above, 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienamide