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Literature summary for 2.5.1.58 extracted from

  • Okolotowicz, K.J.; Lee, W.J.; Hartman, R.F.; Kim, A.Y.; Ottersberg, S.R.; Robinson, D.E., Jr.; Lefler, S.R.; Rose, S.D.
    Inactivation of protein farnesyltransferase by active-site-targeted dicarbonyl compounds (2001), Arch. Pharm., 334, 194-202.
    View publication on PubMed
Search for more literature for 2.5.1.58

Application

Application Comment Organism
medicine prime target for development of anticancer therapeutics Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(+)-6-(camphorquinone-10-sulfonamido)-hexanoic acid
-
 Homo sapiens
(-)-6-(camphorquinone-10-sulfonamido)-hexanoic acid
-
 Homo sapiens
2-oxododecanal
-
 Homo sapiens
4,4-(biphenyldiglyoxaldehyde)
-
 Homo sapiens
5,9,13-trimethyl-8,12-tetradecadiene-2,3-dione 0.093 mM causes a 94% reduction in enzyme activity after 30 min Homo sapiens
5,9-dimethyl-8-decene-2,3-dione 0.017 mM causes a 62% reduction in enzyme activity after 30 min Homo sapiens
dehydrascorbic acid 6-palmitate
-
 Homo sapiens
additional information higher concentrations of the alpha-dicarbonyl compound results in more rapid and more extensive inactivation Homo sapiens
Phenylglyoxal
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
farnesyl diphosphate + protein-cysteine Homo sapiens process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics S-farnesyl protein + diphosphate
-
 ?
farnesyl diphosphate + protein-cysteine Homo sapiens process necessary for the subcellular localisation of substrate to the plasma membrane S-farnesyl protein + diphosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + protein-cysteine
-
 Homo sapiens diphosphate + S-farnesyl protein
-
 ?
farnesyl diphosphate + protein-cysteine process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics Homo sapiens S-farnesyl protein + diphosphate
-
 ?
farnesyl diphosphate + protein-cysteine process necessary for the subcellular localisation of substrate to the plasma membrane Homo sapiens S-farnesyl protein + diphosphate
-
 ?