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Literature summary extracted from

  • Roskoski, R.Jr.; Ritchie, P.
    Role of the carboxyterminal residue in peptide binding to protein farnesyltransferase and protein geranylgeranyltransferase (1998), Arch. Biochem. Biophys., 356, 167-176.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.58
-
Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.58 Cys-Val-Phe-aminohexanoate
-
Rattus norvegicus
2.5.1.58 Cys-Val-Phe-Cys
-
Rattus norvegicus
2.5.1.58 Cys-Val-Phe-Met
-
Rattus norvegicus
2.5.1.58 Cys-Val-Phe-Phe
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Ile-Ile-Met
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Ile-Ala
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Ile-aminohexanoate
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Ile-Cys
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Ile-Gln
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Ile-homoserine
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Ile-Met
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Ile-Phe
-
Rattus norvegicus
2.5.1.58 L-penicillamine-Val-Val-Met
-
Rattus norvegicus
2.5.1.58 additional information tetrapeptides with sequence L-penicillamine-Val-Ile-X and Cys-Val-Phe-X 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 comparison of KM-value of substrates with the structure Lys-Lys-Ser-Ser-Cys-Val-Ile-X for for farnesyltransferase and geranylgeranyltransferase Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.58 farnesyl diphosphate + protein-cysteine Rattus norvegicus
-
S-farnesyl protein + diphosphate
-
?

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 substrate are: Ras superfamiliy and Ras-related proteins for example Rap, Rab, Rac and Ral, large G proteins, nuclear lamins, rhodopsin kinase and the retinal cGMP phosphodiesterase Rattus norvegicus diphosphate + S-farnesyl protein
-
?
2.5.1.58 farnesyl diphosphate + protein-cysteine enzyme prefers linear residues in the X position of the CaaX box over branched residues, enzyme prefers Gln, Met and Ser at the X position Rattus norvegicus diphosphate + S-farnesyl protein
-
?
2.5.1.58 farnesyl diphosphate + protein-cysteine
-
Rattus norvegicus S-farnesyl protein + diphosphate
-
?
2.5.1.58 farnesyl diphosphate + Ras-Cys-Val-Ile-Met best substrate Rattus norvegicus diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
?

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-value of substrates with the structure Lys-Lys-Ser-Ser-Cys-Val-Ile-X for for farnesyltransferase and geranylgeranyltransferase Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.5.1.58 additional information
-
additional information comparison of KI-values of tetrapeptide inhibitors L-penicillamine-Val-Ile-X and Cys-Val-Phe-X for farnesyltransferase and geranylgeranyltransferase Rattus norvegicus
2.5.1.58 0.00008
-
Cys-Val-Phe-Met
-
Rattus norvegicus
2.5.1.58 0.0003
-
L-penicillamine-Val-Ile-Gln
-
Rattus norvegicus
2.5.1.58 0.00052
-
L-penicillamine-Ile-Ile-Met
-
Rattus norvegicus
2.5.1.58 0.0008
-
L-penicillamine-Val-Ile-Cys
-
Rattus norvegicus
2.5.1.58 0.00082
-
L-penicillamine-Val-Val-Met
-
Rattus norvegicus
2.5.1.58 0.0011
-
L-penicillamine-Val-Ile-Met
-
Rattus norvegicus
2.5.1.58 0.0017
-
L-penicillamine-Val-Ile-homoserine
-
Rattus norvegicus
2.5.1.58 0.0028
-
Cys-Val-Phe-Phe
-
Rattus norvegicus
2.5.1.58 0.0029
-
Cys-Val-Phe-Cys
-
Rattus norvegicus
2.5.1.58 0.0034
-
L-penicillamine-Val-Ile-aminohexanoate
-
Rattus norvegicus
2.5.1.58 0.0045
-
L-penicillamine-Val-Ile-Phe
-
Rattus norvegicus
2.5.1.58 0.0053
-
L-penicillamine-Val-Ile-Ala
-
Rattus norvegicus
2.5.1.58 0.0059
-
Cys-Val-Phe-aminohexanoate
-
Rattus norvegicus