Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.5.1.58 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
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
wild-type enzyme and mutant enzymes expressed in Escherichia coli Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
D297A beta-subunit, 200fold decrease in kcat Rattus norvegicus
D297N beta-subunit, 200fold decrease in kcat Rattus norvegicus
H362A beta-subunit, 50fold decrease in kcat Rattus norvegicus
H362Q beta-subunit, 500fold decrease in kcat Rattus norvegicus
H362Q beta-subunit, 15fold decrease in kcat Rattus norvegicus
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]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information wild-type enzyme and the H362E mutant possess similar Km for H-Ras Rattus norvegicus

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ zinc metalloenzyme Rattus norvegicus
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
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

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

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
-
 ?

Turnover Number [1/s]

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