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Literature summary for 2.5.1.59 extracted from

  • Yokoyama, K.; McGeady, P.; Gelb, M.H.
    Mammalian protein geranylgeranyltransferase-I: Substrate specificity, kinetic mechanism, metal requirements, and affinity labeling (1995), Biochemistry, 34, 1344-1354.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-phosphono-(E,E,E)-geranylgeraniol competitive to geranylgeranyl diphosphate, noncompetitive to GST-CDC42 Bos taurus
NPFREKKFFCAIL biotin-gamma6, substrate inhibition at high peptide concentration Bos taurus
PD-083176 noncompetitive to geranylgeranyl diphosphate, competitive to GST-CDC42, modest inhibitor Bos taurus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information comparison of Km of CAAX-substrates with X is Leu, Phe or Ser Bos taurus
0.00027
-
(biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu pH 7.0, 30°C, prenyl donor: geranylgeranyl diphosphate Bos taurus
0.0078
-
(biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu pH 7.0, 30°C, prenyl donor: farnesyl diphosphate Bos taurus
0.016
-
GST-CDC42 pH 7.0, 30°C, prenyl donor: geranylgeranyl diphosphate Bos taurus
0.025
-
(biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu pH 7.0, 30°C, prenyl donor: geranylgeranyl diphosphate Bos taurus

Metals/Ions

Metals/Ions Comment Organism Structure
Cd2+ the zinc in enzyme can be replaced by Cd2+ Bos taurus
Cd2+ 80% of maximal activity in the presence of 0.5 mM alone Bos taurus
Mg2+ 20% of maximal activity in the presence of 0.5 mM alone Bos taurus
Mn2+ 60% of maximal activity in the presence of 0.5 mM alone Bos taurus
additional information not: Co2+ Bos taurus
additional information metals not needed for complex formation between enzyme and geranylgeranyl diphosphate, but addition of prenyl acceptor only results in prenyl transfer in presence of Mg2+ and Zn2+ Bos taurus
Zn2+ required, but no activity in presence of Zn2+ alone, only when either 0.1 mM Mg2+, Mn2+ or Cd2+ is additionally present Bos taurus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
geranylgeranyl diphosphate + protein-cysteine Bos taurus enzyme catalyses the transfer of the 20-carbon prenyl group from geranylgeranyl diphosphate to the cysteine residue near the C-termini of a variety of eukaryotic proteins S-geranylgeranyl-protein + diphosphate
-
?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Bos taurus

Reaction

Reaction Comment Organism Reaction ID
geranylgeranyl diphosphate + protein-cysteine = S-geranylgeranyl-protein + diphosphate random sequential mechanism Bos taurus
geranylgeranyl diphosphate + protein-cysteine = S-geranylgeranyl-protein + diphosphate enzyme and geranylgeranyl diphosphate produce a stable binary complex and the tightly bound geranylgeranyl diphosphate is transferred to a peptide acceptor, without the equilibration of enzyme-bound geranylgeranyl diphosphate with free geranylgeranyl diphosphate Bos taurus
geranylgeranyl diphosphate + protein-cysteine = S-geranylgeranyl-protein + diphosphate this enzyme, along with protein farnesyltransferase, EC 2.5.1.58 and protein geranylgeranyltransferase type II, EC 2.5.1.60, constitutes the protein prenyltransferase family of enzymes Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Bos taurus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu biotin-gamma6 Bos taurus diphosphate + (biotin-CONH-(CH2)5-CO-)-NPFREKKFF-S-farnesyl-CAI-Leu
-
?
geranylgeranyl diphosphate + (biotin-CONH-(CH2)5-CO-)-ALEPPETEPKRKCCIF
-
Bos taurus diphosphate + (biotin-CONH-(CH2)5-CO-)-ALEPPETEPKRK-S-geranylgeranyl-CCIF
-
?
geranylgeranyl diphosphate + (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu biotin-gamma6, preferred substrate Bos taurus diphosphate + (biotin-CONH-(CH2)5-CO-)-NPFREKKFF-S-geranylgeranyl-CAI-Leu
-
?
geranylgeranyl diphosphate + GST-CDC42 recombinant glutathione S-transferase fusion protein of CDC42Hs with a C-terminal Cys-Cys-Ile-Phe sequence Bos taurus diphosphate + GST-S-geranylgeranyl-CDC42
-
?
geranylgeranyl diphosphate + protein-cysteine enzyme requires that protein substrates contain a Cys residue fourth from the C terminus, protein substrate motif: Cys-aliphatic-aliphatic-X. X is Leu, Phe or Ser, preferred substrate: Leu Bos taurus S-geranylgeranyl-protein + diphosphate
-
?
geranylgeranyl diphosphate + protein-cysteine enzyme requires that protein substrates contain a Cys residue fourth from the C terminus, protein substrate motif: Cys-aliphatic-aliphatic-X. X may be Leu, Phe, or Ser, with high concentrations of peptide substrates this specificity is lost Bos taurus S-geranylgeranyl-protein + diphosphate
-
?
geranylgeranyl diphosphate + protein-cysteine enzyme catalyses the transfer of the 20-carbon prenyl group from geranylgeranyl diphosphate to the cysteine residue near the C-termini of a variety of eukaryotic proteins Bos taurus S-geranylgeranyl-protein + diphosphate
-
?

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 CAAX-substrates with X is Leu, Phe or Ser Bos taurus
0.0057
-
GST-CDC42 prenyl donor: geranylgeranyl diphosphate Bos taurus
0.028
-
(biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu prenyl donor: geranylgeranyl diphosphate Bos taurus
0.1
-
(biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu prenyl donor: farnesyl diphosphate Bos taurus
0.12
-
(biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu prenyl donor: geranylgeranyl diphosphate Bos taurus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00072
-
1-phosphono-(E,E,E)-geranylgeraniol with respect to geranylgeranyl diphosphate Bos taurus
0.00086
-
1-P-GGOH with respect to GST-CDC42 Bos taurus
0.0082
-
PD-083176 with respect to GST-CDC42 Bos taurus
0.0087
-
PD-083176 with respect to geranylgeranyl diphosphate Bos taurus