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Literature summary for 2.5.1.58 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
Search for more literature for 2.5.1.58

Inhibitors

Inhibitors Comment Organism Structure
(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
(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
(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
(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
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
-
 Homo sapiens
(4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
-
 Saccharomyces cerevisiae
(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienamide
-
 Homo sapiens
(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
(4E,8E)-N-hydroxy-5,9,13-trimethyltetradeca-4,8,12-trienamide
-
 Homo sapiens
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
-
 Homo sapiens
(6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
-
 Saccharomyces cerevisiae
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
-
 Homo sapiens
(7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
-
 Saccharomyces cerevisiae
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
-
 Homo sapiens
3-oxo-3-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanoic acid
-
 Saccharomyces cerevisiae
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
-
 Homo sapiens
4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
-
 Saccharomyces cerevisiae
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
-
 Homo sapiens
5-oxo-5-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]pentanoic acid
-
 Saccharomyces cerevisiae
chaetomellic acid A
-
 Homo sapiens
chaetomellic acid A
-
 Saccharomyces cerevisiae
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
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
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
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
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
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
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
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
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
-
 Homo sapiens
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
-
 Saccharomyces cerevisiae
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Homo sapiens
[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Saccharomyces cerevisiae
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
-
 Homo sapiens
[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
-
 Saccharomyces cerevisiae
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Homo sapiens
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Plasmodium falciparum
[3-(1-methyl-1H-imidazol-2-yl)propyl][(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
-
 Trypanosoma brucei
[[(2E,4E,8E)-5,9,13-trimethyltetradeca-2,4,8,12-tetraenoyl]amino]propanedioic acid
-
 Saccharomyces cerevisiae
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
-
 Homo sapiens
[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
-
 Saccharomyces cerevisiae
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
-
 Homo sapiens
[[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
-
 Saccharomyces cerevisiae

Organism

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

Synonyms

Synonyms Comment Organism
FTase
-
 Homo sapiens
FTase
-
 Saccharomyces cerevisiae
FTase
-
 Trypanosoma brucei
FTase
-
 Plasmodium falciparum
protein farnesyltransferase
-
 Homo sapiens
protein farnesyltransferase
-
 Saccharomyces cerevisiae
protein farnesyltransferase
-
 Trypanosoma brucei
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
30
-
 assay at Trypanosoma brucei
30
-
 assay at Plasmodium falciparum

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000175
-
 30°C, pH 7.5 Homo sapiens chaetomellic acid A
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
0.00034
-
 30°C, pH 7.5 Saccharomyces cerevisiae chaetomellic acid A
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
0.00088
-
 30°C, pH 7.5 Homo sapiens [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
0.0009
-
 30°C, pH 7.5 Homo sapiens [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ylidene]propanedioic acid
0.004
-
 30°C, pH 7.5 Saccharomyces cerevisiae [(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]propanedioic acid
0.005
-
 30°C, pH 7.5 Saccharomyces cerevisiae [[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
0.01
-
 30°C, pH 7.5 Homo sapiens [[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]propanedioic acid
0.015
-
 30°C, pH 7.5 Saccharomyces cerevisiae (7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
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
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
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
0.06
-
 30°C, pH 7.5 Homo sapiens (7E,11E)-8,12,16-trimethyl-4-oxoheptadeca-7,11,15-trienoic acid
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
0.06
-
 30°C, pH 7.5 Homo sapiens [[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
0.08
-
 30°C, pH 7.5 Saccharomyces cerevisiae (6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
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
0.085
-
 30°C, pH 7.5 Homo sapiens [(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
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
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 Homo sapiens 4-oxo-4-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy]butanoic acid
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
0.17
-
 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoic acid
0.2
-
 30°C, pH 7.5 Saccharomyces cerevisiae (4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
0.2
-
 30°C, pH 7.5 Homo sapiens (6E,10E)-7,11,15-trimethyl-3-oxohexadeca-6,10,14-trienoic acid
0.2
-
 30°C, pH 7.5 Saccharomyces cerevisiae [(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]sulfamic acid
0.2
-
 30°C, pH 7.5 Saccharomyces cerevisiae [[(4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoyl]amino]propanedioic acid
0.2
-
 value above, 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyl-N-(phenylsulfonyl)tetradeca-4,8,12-trienamide
0.2
-
 value above, 30°C, pH 7.5 Homo sapiens (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienamide