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Literature summary extracted from

  • Fu, H.W.; Beese, L.S.; Casey, P.J.
    Kinetic analysis of zinc ligand mutants of mammalian protein farnesyltransferase (1998), Biochemistry, 37, 4465-4472.
    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

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.58 wild-type enzyme and mutant enzymes expressed in Escherichia coli Rattus norvegicus

Protein Variants

EC Number Protein Variants Comment Organism
2.5.1.58 D297A beta-subunit, 200fold decrease in kcat Rattus norvegicus
2.5.1.58 D297N beta-subunit, 200fold decrease in kcat Rattus norvegicus
2.5.1.58 H362A beta-subunit, 50fold decrease in kcat Rattus norvegicus
2.5.1.58 H362Q beta-subunit, 500fold decrease in kcat Rattus norvegicus
2.5.1.58 H362Q beta-subunit, 15fold decrease in kcat Rattus norvegicus
2.5.1.58 additional information all five mutant enzymes bind farnesyl diphosphate with similar affinity to that of the wild-type enzyme, indicating that the targeted residues neither directly nor indirectly influence the farnesyl diphosphate binding site, only the wild-type enzyme able to bind zinc, while all five of the mutant enzymes lose this ability 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 wild-type enzyme and the H362E mutant possess similar Km for H-Ras Rattus norvegicus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.5.1.58 Zn2+ zinc metalloenzyme Rattus norvegicus
2.5.1.58 Zn2+ zinc ion is coordinated by three residues in the beta subunit: Asp-297, Cys-299, and H-362 and a water molecule Rattus norvegicus
2.5.1.58 Zn2+ zinc plays a major catalytic role in the mechanism of enzyme, zinc seems to activate the cysteine thiol of protein substrate for attack at C-1 of the isoprenoid substrate Rattus norvegicus

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.58 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
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.5.1.58 additional information
-
 additional information comparison of kcat of wild-type and mutant enzymes Rattus norvegicus