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Literature summary extracted from

  • Yokoyama, K.; Trobridge, P.; Buckner, F.S.; Van Voorhis, W.C.; Stuart, K.D.; Gelb, M.H.
    Protein farnesyltransferase from Trypanosoma brucei. A heterodimer of 61- and 65-kDa subunits as a new target for antiparasite therapeutics (1998), J. Biol. Chem., 273, 26497-26505.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.5.1.58 medicine prime target for development of anticancer therapeutics Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.58 FTI-276 about 2fold more potent on parasite enzyme than on mammalian enzyme Rattus norvegicus
2.5.1.58 FTI-276 about 2fold more potent on parasite enzyme than on mammalian enzyme Trypanosoma brucei brucei
2.5.1.58 FTI-277 inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei completely inhibited with 0.001 mM Rattus norvegicus
2.5.1.58 FTI-277 inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei completely inhibited with 0.001 mM Trypanosoma brucei brucei
2.5.1.58 GGTI-297 inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme Rattus norvegicus
2.5.1.58 GGTI-297 inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme Trypanosoma brucei brucei
2.5.1.58 GGTI-298 inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei cmpletely inhibited with 0.005 mM Rattus norvegicus
2.5.1.58 GGTI-298 inhibition with potencies 10fold higher on parasite enzyme than on mammalian enzyme, however growth of bloodstream Trypanosoma brucei cmpletely inhibited with 0.005 mM Trypanosoma brucei brucei
2.5.1.58 L-745,631 similarly potent on parasite enzyme and on mammalian enzyme Rattus norvegicus
2.5.1.58 L-745,631 similarly potent on parasite enzyme and on mammalian enzyme Trypanosoma brucei brucei
2.5.1.58 SCH-44342 2 orders of magnitude less potent on parasite enzyme than on mammalian enzyme Rattus norvegicus
2.5.1.58 SCH-44342 2 orders of magnitude less potent on parasite enzyme than on mammalian enzyme Trypanosoma brucei brucei

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.5.1.58 61000
-
 alpha,beta, 1 * 61000 + 1 * 65000, SDS-PAGE Trypanosoma brucei brucei
2.5.1.58 65000
-
 alpha,beta, 1 * 61000 + 1 * 65000, SDS-PAGE Trypanosoma brucei brucei

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.58 Rattus norvegicus
-
-
-
2.5.1.58 Trypanosoma brucei brucei
-
 EATRO 140
-
2.5.1.58 Trypanosoma brucei brucei EATRO 140
-
 EATRO 140
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.58
-
 Trypanosoma brucei brucei

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.5.1.58 procyclic form
-
 Trypanosoma brucei brucei
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.5.1.58 13.5
-
-
 Trypanosoma brucei brucei

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.58 farnesyl diphosphate + protein-cysteine Ha-Ras-CVLS, which is a good substrate for mammalian enzyme, not farnesylated by the parasite enzyme, only the mammalian enzyme substrate RAS1-CVIM farnesylated by parasite enzyme Rattus norvegicus diphosphate + S-farnesyl protein
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine Ha-Ras-CVLS, which is a good substrate for mammalian enzyme, not farnesylated by the parasite enzyme, only the mammalian enzyme substrate RAS1-CVIM farnesylated by parasite enzyme Trypanosoma brucei brucei diphosphate + S-farnesyl protein
-
 ?
2.5.1.58 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
-
 ?
2.5.1.58 farnesyl diphosphate + protein-cysteine Ha-Ras-CVLS, which is a good substrate for mammalian enzyme, not farnesylated by the parasite enzyme, only the mammalian enzyme substrate RAS1-CVIM farnesylated by parasite enzyme Trypanosoma brucei brucei EATRO 140 diphosphate + S-farnesyl protein
-
 ?
2.5.1.58 farnesyl diphosphate + Ras-Cys-Val-Ile-Met
-
 Rattus norvegicus diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
 ?
2.5.1.58 farnesyl diphosphate + Ras-Cys-Val-Ile-Met
-
 Trypanosoma brucei brucei diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
 ?
2.5.1.58 farnesyl diphosphate + Ras-Cys-Val-Ile-Met
-
 Trypanosoma brucei brucei EATRO 140 diphosphate + Ras-S-farnesyl-Cys-Val-Ile-Met
-
 ?

Subunits

EC Number Subunits Comment Organism
2.5.1.58 heterodimer
-
 Rattus norvegicus
2.5.1.58 heterodimer alpha,beta, 1 * 61000 + 1 * 65000, SDS-PAGE Trypanosoma brucei brucei