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Literature summary for 2.5.1.58 extracted from

  • Subramanian, T.; Pais, J.E.; Liu, S.; Troutman, J.M.; Suzuki, Y.; Leela Subramanian, K.; Fierke, C.A.; Andres, D.A.; Spielmann, H.P.
    Farnesyl diphosphate analogues with aryl moieties are efficient alternate substrates for protein farnesyltransferase (2012), Biochemistry, 51, 8307-8319.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0005
-
(E)-[4-[(3,7-dimethylocta-2,6-dien-1-yl)oxy]phenyl]-methanyl diphosphate pH 7.8, 25°C Rattus norvegicus
0.0015
-
(2E,6E)-farnesyl diphosphate pH 7.8, 25°C Rattus norvegicus
0.0015
-
[3-[(3-phenoxyphenoxy)methyl]phenyl]-methanyl diphosphate pH 7.8, 25°C Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dansyl-GCVLS + (2E,6E)-farnesyl diphosphate
-
Rattus norvegicus dansyl-G-(S-(2E,6E)-farnesyl)CVLS + diphosphate
-
?
dansyl-GCVLS + (E)-[4-[(3,7-dimethylocta-2,6-dien-1-yl)oxy]phenyl]-methanyl diphosphate
-
Rattus norvegicus dansyl-G-(S-(E)-[4-[(3,7-dimethylocta-2,6-dien-1-yl)oxy]phenyl]-methanyl)CVLS + diphosphate
-
?
dansyl-GCVLS + [3-[(3-phenoxyphenoxy)methyl]phenyl]-methanyl diphosphate
-
Rattus norvegicus dansyl-G-(S-[3-[(3-phenoxyphenoxy)methyl]phenyl]-methanyl)CVLS + diphosphate
-
?
additional information steady-state kinetics for modification of peptide substrates shows that the multiple-turnover activity depends on the analogue structure. Analogues in which the first isoprene is replaced with a benzyl group and an analogue in which each isoprene is replaced with an aryl group are good substrates. The single-turnover rate constant for alkylation depends on the Ca1a2X peptide sequence. The isoprenoid transition-state conformation is preferred over the inactive E-FPP-Ca1a2X ternary complex conformation and the farnesyl binding site in the exit groove may be significantly more selective for the farnesyl diphosphate substrate than the active site binding pocket Rattus norvegicus ?
-
?

Synonyms

Synonyms Comment Organism
FTase
-
Rattus norvegicus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.053
-
(E)-[4-[(3,7-dimethylocta-2,6-dien-1-yl)oxy]phenyl]-methanyl diphosphate pH 7.8, 25°C Rattus norvegicus
0.29
-
(2E,6E)-farnesyl diphosphate pH 7.8, 25°C Rattus norvegicus
0.29
-
[3-[(3-phenoxyphenoxy)methyl]phenyl]-methanyl diphosphate pH 7.8, 25°C Rattus norvegicus

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
110
-
(E)-[4-[(3,7-dimethylocta-2,6-dien-1-yl)oxy]phenyl]-methanyl diphosphate pH 7.8, 25°C Rattus norvegicus
193
-
(2E,6E)-farnesyl diphosphate pH 7.8, 25°C Rattus norvegicus
300
-
[3-[(3-phenoxyphenoxy)methyl]phenyl]-methanyl diphosphate pH 7.8, 25°C Rattus norvegicus