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Literature summary extracted from

  • Micali, E.; Chehade, K.A.; Isaacs, R.J.; Andres, D.A.; Spielmann, H.P.
    Protein farnesyltransferase isoprenoid substrate discrimination is dependent on isoprene double bonds and branched methyl groups (2001), Biochemistry, 40, 12254-12265.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.5.1.58 medicine evidence that inhibitors of enzyme could be effective therapeutic agents in treatment of many human cancers Rattus norvegicus
2.5.1.58 medicine prime target for development of anticancer therapeutics Rattus norvegicus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.58 expression in Escherichia coli Rattus norvegicus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.5.1.58 X-ray crystal structure, modelling indicates that geranylgeranyl diphosphate adopts a different conformation than the farnesyl chain of farnesyl diphosphate Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.5.1.58 additional information
-
 additional information correlation between Km and analogue hydrophobicity and length Rattus norvegicus
2.5.1.58 0.046
-
 farnesyl diphosphate
-
 Rattus norvegicus
2.5.1.58 0.056
-
 8-benzyloxy-3-methyl-2-octen-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 0.089
-
 10-benzyloxy-3-methyl-2-decen-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 0.091
-
 9-benzyloxy-3-methyl-2-nonen-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 0.13
-
 7-benzyloxy-3-methyl-2-hepten-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 0.45
-
 geranylgeranyl diphosphate
-
 Rattus norvegicus
2.5.1.58 0.89
-
 6-benzyloxy-3-methyl-2-hexen-1-ol-diphosphate
-
 Rattus norvegicus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.5.1.58 Mg2+ required Rattus norvegicus
2.5.1.58 Mg2+ appears to coordinate the diphosphate moiety of farnesyl diphosphate Rattus norvegicus
2.5.1.58 Zn2+ required Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.58 farnesyl diphosphate + protein-cysteine Rattus norvegicus process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics S-farnesyl protein + diphosphate
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine Rattus norvegicus process necessary for the subcellular localisation of substrate to the plasma membrane S-farnesyl protein + diphosphate
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine Rattus norvegicus enzyme responsible for catalysing isoprene lipid modifications S-farnesyl protein + diphosphate
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine Rattus norvegicus A series of steps modifies the C-terminus of Ras. Enzyme catalyses the first of these steps by transferring the farnesyl group from farnesyl diphosphates to the cysteine side chain in the CAAX sequence motif at the C-terminus of Ras S-farnesyl protein + diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.58 Rattus norvegicus
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
2.5.1.58 farnesyl diphosphate + protein-cysteine = S-farnesyl protein + diphosphate kinetic mechanism Rattus norvegicus
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.58 10-benzyloxy-3-methyl-2-decen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
-
 Rattus norvegicus diphosphate + N-dansyl-Gly-S-(10-benzyloxy-3-methyl-2-decenyl)-Cys-Val-Leu-Ser
-
 ?
2.5.1.58 6-benzyloxy-3-methyl-2-hexen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
-
 Rattus norvegicus diphosphate + N-dansyl-Gly-S-(6-benzyloxy-3-methyl-2-hexenyl)-Cys-Val-Leu-Ser
-
 ?
2.5.1.58 7-benzyloxy-3-methyl-2-hepten-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
-
 Rattus norvegicus diphosphate + N-dansyl-Gly-S-(7-benzyloxy-3-methyl-2-heptenyl)-Cys-Val-Leu-Ser
-
 ?
2.5.1.58 8-benzyloxy-3-methyl-2-octen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
-
 Rattus norvegicus diphosphate + N-dansyl-Gly-S-(8-benzyloxy-3-methyl-2-octenyl)-Cys-Val-Leu-Ser
-
 ?
2.5.1.58 9-benzyloxy-3-methyl-2-nonen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
-
 Rattus norvegicus diphosphate + N-dansyl-Gly-S-(9-benzyloxy-3-methyl-2-nonenyl)-Cys-Val-Leu-Ser
-
 ?
2.5.1.58 farnesyl diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser the best substrate Rattus norvegicus diphosphate + N-dansyl-Gly-S-farnesyl-Cys-Val-Leu-Ser
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln Rattus norvegicus diphosphate + S-farnesyl protein
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics Rattus norvegicus S-farnesyl protein + diphosphate
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine process necessary for the subcellular localisation of substrate to the plasma membrane Rattus norvegicus S-farnesyl protein + diphosphate
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine enzyme responsible for catalysing isoprene lipid modifications Rattus norvegicus S-farnesyl protein + diphosphate
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine A series of steps modifies the C-terminus of Ras. Enzyme catalyses the first of these steps by transferring the farnesyl group from farnesyl diphosphates to the cysteine side chain in the CAAX sequence motif at the C-terminus of Ras Rattus norvegicus S-farnesyl protein + diphosphate
-
 ?
2.5.1.58 geranylgeranyl diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser
-
 Rattus norvegicus diphosphate + N-dansyl-Gly-S-geranylgeranyl-Cys-Val-Leu-Ser
-
 ?
2.5.1.58 geranylgeranyl diphosphate + protein-cysteine
-
 Rattus norvegicus diphosphate + S-geranylgeranylcysteinyl protein
-
 ?
2.5.1.58 additional information not: geranylgeranyl diphosphate Rattus norvegicus ?
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.5.1.58 0.84
-
 7-benzyloxy-3-methyl-2-hepten-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 15
-
 geranylgeranyl diphosphate
-
 Rattus norvegicus
2.5.1.58 25
-
 10-benzyloxy-3-methyl-2-decen-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 27
-
 8-benzyloxy-3-methyl-2-octen-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 43
-
 9-benzyloxy-3-methyl-2-nonen-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 44
-
 6-benzyloxy-3-methyl-2-hexen-1-ol-diphosphate
-
 Rattus norvegicus
2.5.1.58 100
-
 farnesyl diphosphate
-
 Rattus norvegicus