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Literature summary 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

EC Number Inhibitors Comment Organism Structure
2.5.1.59 1-phosphono-(E,E,E)-geranylgeraniol competitive to geranylgeranyl diphosphate, noncompetitive to GST-CDC42 Bos taurus
2.5.1.59 NPFREKKFFCAIL biotin-gamma6, substrate inhibition at high peptide concentration Bos taurus
2.5.1.59 PD-083176 noncompetitive to geranylgeranyl diphosphate, competitive to GST-CDC42, modest inhibitor Bos taurus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.5.1.59 additional information
-
 additional information comparison of Km of CAAX-substrates with X is Leu, Phe or Ser Bos taurus
2.5.1.59 0.00027
-
 (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu pH 7.0, 30°C, prenyl donor: geranylgeranyl diphosphate Bos taurus
2.5.1.59 0.0078
-
 (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu pH 7.0, 30°C, prenyl donor: farnesyl diphosphate Bos taurus
2.5.1.59 0.016
-
 GST-CDC42 pH 7.0, 30°C, prenyl donor: geranylgeranyl diphosphate Bos taurus
2.5.1.59 0.025
-
 (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu pH 7.0, 30°C, prenyl donor: geranylgeranyl diphosphate Bos taurus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.5.1.59 Cd2+ the zinc in enzyme can be replaced by Cd2+ Bos taurus
2.5.1.59 Cd2+ 80% of maximal activity in the presence of 0.5 mM alone Bos taurus
2.5.1.59 Mg2+ 20% of maximal activity in the presence of 0.5 mM alone Bos taurus
2.5.1.59 Mn2+ 60% of maximal activity in the presence of 0.5 mM alone Bos taurus
2.5.1.59 additional information not: Co2+ Bos taurus
2.5.1.59 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
2.5.1.59 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)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.59 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

EC Number Organism UniProt Comment Textmining
2.5.1.59 Bos taurus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.59
-
 Bos taurus

Reaction

EC Number Reaction Comment Organism Reaction ID
2.5.1.59 geranylgeranyl diphosphate + protein-cysteine = S-geranylgeranyl-protein + diphosphate random sequential mechanism Bos taurus
a
2.5.1.59 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
a
2.5.1.59 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
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.5.1.59 brain
-
 Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.59 farnesyl diphosphate + (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu biotin-gamma6 Bos taurus diphosphate + (biotin-CONH-(CH2)5-CO-)-NPFREKKFF-S-farnesyl-CAI-Leu
-
 ?
2.5.1.59 geranylgeranyl diphosphate + (biotin-CONH-(CH2)5-CO-)-ALEPPETEPKRKCCIF
-
 Bos taurus diphosphate + (biotin-CONH-(CH2)5-CO-)-ALEPPETEPKRK-S-geranylgeranyl-CCIF
-
 ?
2.5.1.59 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
-
 ?
2.5.1.59 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
-
 ?
2.5.1.59 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
-
 ?
2.5.1.59 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
-
 ?
2.5.1.59 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]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.5.1.59 additional information
-
 additional information comparison of kcat of CAAX-substrates with X is Leu, Phe or Ser Bos taurus
2.5.1.59 0.0057
-
 GST-CDC42 prenyl donor: geranylgeranyl diphosphate Bos taurus
2.5.1.59 0.028
-
 (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu prenyl donor: geranylgeranyl diphosphate Bos taurus
2.5.1.59 0.1
-
 (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu prenyl donor: farnesyl diphosphate Bos taurus
2.5.1.59 0.12
-
 (biotin-CONH-(CH2)5-CO-)-NPFREKKFFCAI-Leu prenyl donor: geranylgeranyl diphosphate Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.5.1.59 0.00072
-
 1-phosphono-(E,E,E)-geranylgeraniol with respect to geranylgeranyl diphosphate Bos taurus
2.5.1.59 0.00086
-
 1-P-GGOH with respect to GST-CDC42 Bos taurus
2.5.1.59 0.0082
-
 PD-083176 with respect to GST-CDC42 Bos taurus
2.5.1.59 0.0087
-
 PD-083176 with respect to geranylgeranyl diphosphate Bos taurus