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Literature summary for 2.5.1.58 extracted from

  • Hast, M.A.; Fletcher, S.; Cummings, C.G.; Pusateri, E.E.; Blaskovich, M.A.; Rivas, K.; Gelb, M.H.; Van Voorhis, W.C.; Sebti, S.M.; Hamilton, A.D.; Beese, L.S.
    Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase (2009), Chem. Biol., 16, 181-192.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
-
Homo sapiens
-
Rattus norvegicus
-
Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
-
Homo sapiens
3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
-
Plasmodium falciparum
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
-
Homo sapiens
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
-
Plasmodium falciparum
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
-
Homo sapiens
N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
-
Plasmodium falciparum
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
Plasmodium falciparum
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens
-
Rattus norvegicus
-
Plasmodium falciparum

Synonyms

Synonyms Comment Organism
FTase
-
Homo sapiens
FTase
-
Rattus norvegicus
FTase
-
Plasmodium falciparum
hFTase
-
Homo sapiens
protein farnesyltransferase
-
Homo sapiens
protein farnesyltransferase
-
Rattus norvegicus
protein farnesyltransferase
-
Plasmodium falciparum
rFTase
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000005
-
-
Plasmodium falciparum N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
0.0000012
-
-
Plasmodium falciparum tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
0.000003
-
-
Plasmodium falciparum tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate
0.000005
-
-
Plasmodium falciparum N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
0.000056
-
-
Homo sapiens N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-1-methyl-1H-imidazole-4-sulfonamide
0.00007
-
-
Plasmodium falciparum 3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
0.00016
-
-
Homo sapiens N-(1-benzyl-2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl)-2-methylbenzenesulfonamide
0.0008
-
-
Homo sapiens 3-[3-[2-([2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1-([(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]methyl)ethyl]sulfamoyl)benzyl]phenyl]propanoic acid
0.0037
-
-
Homo sapiens tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]propyl)piperidine-1-carboxylate
0.00405
-
-
Homo sapiens tert-butyl 4-(3-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]-2-[[(2-methylphenyl)sulfonyl]amino]propyl)piperidine-1-carboxylate

General Information

General Information Comment Organism
physiological function posttranslational modification of proteins involved in intracellular signal transduction network Homo sapiens
physiological function posttranslational modification of proteins involved in intracellular signal transduction network Rattus norvegicus
physiological function posttranslational modification of proteins involved in intracellular signal transduction network Plasmodium falciparum