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Literature summary for 2.5.1.58 extracted from

  • Huang, C.c.; Hightower, K.E.; Fierke, C.A.
    Mechanistic studies of rat protein farnesyltransferase indicate an associative transition state (2000), Biochemistry, 39, 2593-2602.
    View publication on PubMed
Search for more literature for 2.5.1.58

Application

Application Comment Organism
medicine evidence that inhibitors of enzyme could be effective therapeutic agents in treatment of many human cancers Rattus norvegicus

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Rattus norvegicus

Metals/Ions

Metals/Ions Comment Organism Structure
Cd2+ substitution of the active site zinc with cadmium increases the affinity of the peptide substrate and decreases the rate constant for the chemical step Rattus norvegicus
Mg2+ magnesium is not required for formation of the thioether product but the presence increases the single-turnover rate constant by several orders of magnitude at saturating enzyme and substrate concentrations Rattus norvegicus
Mg2+ appears to coordinate the diphosphate moiety of farnesyl diphosphate Rattus norvegicus
additional information a metal-assisted nucleophile is involved in the catalytic mechanism of enzyme Rattus norvegicus
Zn2+ zinc metalloenzyme Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
farnesyl diphosphate + protein-cysteine Rattus norvegicus process necessary for the subcellular localisation of substrate to the plasma membrane S-farnesyl protein + diphosphate
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 ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
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-
-

Reaction

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + protein-cysteine prenylation, farnesylation, substrates are Ras, nuclear lamins, transducin gamma subunit, protein substrate motif: Cys-aliphatic-aliphatic-X, X: M, S, Q, A, F Rattus norvegicus diphosphate + S-farnesyl protein
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 ?
farnesyl diphosphate + protein-cysteine process necessary for the subcellular localisation of substrate to the plasma membrane Rattus norvegicus S-farnesyl protein + diphosphate
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 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
additional information
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 additional information comparison of kcat of metal-substituted enzymes, kcat for product formation decreases for C3 fluoromethyl farnesyl diphosphate substrates, paralleling the number of fluorines at the C3 methyl position Rattus norvegicus