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Literature summary extracted from

  • Machida, S.; Usuba, K.; Blaskovich, M.A.; Yano, A.; Harada, K.; Sebti, S.M.; Kato, N.; Ohkanda, J.
    Module assembly for protein-surface recognition: geranylgeranyltransferase I bivalent inhibitors for simultaneous targeting of interior and exterior protein surfaces (2008), Chemistry, 14, 1392-1401.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.59 expressed in Escherichia coli BL21 (DE3) and Sf9 insect cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.59 11-aminoundecylcarbonyl-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine competitive. bivalent inhibitor for simultaneous recognition of both exteriorand interior protein surface. Not inhibitory against farnesyltransferase Rattus norvegicus
2.5.1.59 L-cysteinyl-L-valyl-L-isoleucyl-L-leucine
-
 Homo sapiens
2.5.1.59 additional information not inhibited by 3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoic acid methyl ester trifluoroacetate and mono(3,3',3''-(5-(methoxycarbonyl)benzene-1,2,3-triyl)tris(oxy)tripropan-1-aminium) mono(2,2,2-trifluoroacetate) Homo sapiens
2.5.1.59 N-(12-ammoniododecanoyl)-D-cysteinyl-L-valyl-L-isoleucyl-L-leucine trifluoroacetate
-
 Homo sapiens
2.5.1.59 N-(12-[[(3-[[(3R)-3-ammonio-4-phenylbutyl]oxy]-4,5-bis[[(3S)-3-ammonio-4-phenylbutyl]oxy]phenyl)carbonyl]amino]dodecanoyl)-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)
-
 Homo sapiens
2.5.1.59 N-(4-[[(3-[[(3R)-3-ammonio-4-phenylbutyl]oxy]-4,5-bis[[(3S)-3-ammonio-4-phenylbutyl]oxy]phenyl)carbonyl]amino]butanoyl)-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)
-
 Homo sapiens
2.5.1.59 N-[12-([[3,4,5-tris(3-ammoniopropoxy)phenyl]carbonyl]amino)dodecanoyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)
-
 Homo sapiens
2.5.1.59 N-[6-(3,4,5-tris(3-amino-1-propoxy)benzoylamino)-undecylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine competitive, bivalent inhibitor for simultaneous recognition of both exterior and interior protein surface. Not inhibitory against farnesyltransferase Rattus norvegicus
2.5.1.59 N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-hexylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine trifluoroacetate
-
 Homo sapiens
2.5.1.59 N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-propylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine bivalent inhibitor for simultaneous recognition of both exterior and interior protein surface. Not inhibitory against farnesyltransferase Rattus norvegicus
2.5.1.59 N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-undecylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine competitive, bivalent inhibitor for simultaneous recognition of both exterior and interior protein surface. Not inhibitory against farnesyltransferase Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.59 Homo sapiens
-
-
-
2.5.1.59 Rattus norvegicus
-
 type I enzyme
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.59 nickel agarose resin chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.59 geranylgeranyl diphosphate + N-dansyl-Gly-Cys-Val-Ile-Leu-OH
-
 Rattus norvegicus ?
-
 ?
2.5.1.59 geranylgeranyl diphosphate + protein-cysteine
-
 Homo sapiens S-geranylgeranyl-protein + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.59 geranylgeranyltransferase I
-
 Homo sapiens
2.5.1.59 GGTase type I enzyme Rattus norvegicus
2.5.1.59 GGTase I
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.59 0.0006
-
-
 Homo sapiens N-[12-([[3,4,5-tris(3-ammoniopropoxy)phenyl]carbonyl]amino)dodecanoyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)
2.5.1.59 0.0006
-
-
 Rattus norvegicus N-[6-(3,4,5-tris(3-amino-1-propoxy)benzoylamino)-undecylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine
2.5.1.59 0.00064
-
-
 Rattus norvegicus N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-undecylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine
2.5.1.59 0.00066
-
-
 Homo sapiens N-(4-[[(3-[[(3R)-3-ammonio-4-phenylbutyl]oxy]-4,5-bis[[(3S)-3-ammonio-4-phenylbutyl]oxy]phenyl)carbonyl]amino]butanoyl)-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)
2.5.1.59 0.00066
-
-
 Rattus norvegicus N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-propylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine
2.5.1.59 0.00098
-
-
 Rattus norvegicus N-[6-(3,4,5-tris(3-amino-4-phenyl-1-butoxy)benzoylamino)-undecylcarbonyl]-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine
2.5.1.59 0.00098
-
-
 Homo sapiens N-(12-[[(3-[[(3R)-3-ammonio-4-phenylbutyl]oxy]-4,5-bis[[(3S)-3-ammonio-4-phenylbutyl]oxy]phenyl)carbonyl]amino]dodecanoyl)-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine tris(trifluoroacetate)
2.5.1.59 0.0014
-
-
 Homo sapiens N-(12-ammoniododecanoyl)-D-cysteinyl-L-valyl-L-isoleucyl-L-leucine trifluoroacetate
2.5.1.59 0.0014
-
-
 Rattus norvegicus 11-aminoundecylcarbonyl-L-cysteinyl-L-valyl-L-isoleucyl-L-leucine
2.5.1.59 0.0048
-
-
 Homo sapiens L-cysteinyl-L-valyl-L-isoleucyl-L-leucine