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Literature summary extracted from

  • Ibrahim, M.; Azzouz, N.; Gerold, P.; Schwarz, R.T.
    Identification and characterisation of Toxoplasma gondii protein farnesyltransferase (2001), Int. J. Parasitol., 31, 1489-1497.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.5.1.58 medicine prime target for development of anticancer therapeutics Homo sapiens
2.5.1.58 medicine prime target for development of anticancer therapeutics Toxoplasma gondii
2.5.1.58 medicine possibility of development of specific inhibitors for parasitic protozoa Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.58 farnesyltransferase inhibitors I and II peptidomimemtic inhibitors, inhibitor I: 50% inhibition at 270 nM, inhibitor II: 50% inhibition at 0.97 nM Toxoplasma gondii
2.5.1.58 KTSCVAM 40% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells Homo sapiens
2.5.1.58 KTSCVAM 40% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells Toxoplasma gondii
2.5.1.58 KTSCVFM 80% inhibition of farnesylation in Toxoplasma gondii and 80% inhibition of enzyme in HeLa cells Homo sapiens
2.5.1.58 KTSCVFM 80% inhibition of farnesylation in Toxoplasma gondii and 80% inhibition of enzyme in HeLa cells Toxoplasma gondii
2.5.1.58 KTSCVIA 50% inhibition of farnesylation in Toxoplasma gondii and no inhibition of enzyme in HeLa cells Homo sapiens
2.5.1.58 KTSCVIA 50% inhibition of farnesylation in Toxoplasma gondii and no inhibition of enzyme in HeLa cells Toxoplasma gondii
2.5.1.58 KTSCVIF no inhibition of farnesylation in Toxoplasma gondii, 80% inhibition of enzyme in HeLa cells Homo sapiens
2.5.1.58 KTSCVIF no inhibition of farnesylation in Toxoplasma gondii, 80% inhibition of enzyme in HeLa cells Toxoplasma gondii
2.5.1.58 KTSSVIM 80% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells Homo sapiens
2.5.1.58 KTSSVIM 80% inhibition of farnesylation in Toxoplasma gondii, 100% inhibition of enzyme in HeLa cells Toxoplasma gondii
2.5.1.58 additional information not: KTSSVIM Homo sapiens
2.5.1.58 additional information not: KTSSVIM Toxoplasma gondii

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.5.1.58 Mg2+ required Toxoplasma gondii
2.5.1.58 additional information not: Ca2+ Toxoplasma gondii
2.5.1.58 Zn2+ required Toxoplasma gondii
2.5.1.58 Zn2+ optimal activity in the presence of 0.025 mM Homo sapiens
2.5.1.58 Zn2+ optimal activity in the presence of 0.025 mM Toxoplasma gondii

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 Toxoplasma gondii enzyme responsible for catalysing isoprene lipid modifications S-farnesyl protein + diphosphate
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.58 Homo sapiens
-
mammalian HeLa cells
-
2.5.1.58 Toxoplasma gondii
-
tachyzoites of the RH strain were grown and maintained in Cercopithecus aethiops kidney cells
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.58
-
Toxoplasma gondii

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.58 farnesyl diphosphate + protein-cysteine
-
Homo sapiens diphosphate + S-farnesyl protein
-
?
2.5.1.58 farnesyl diphosphate + protein-cysteine substrate: Biotin lamin-B protein Toxoplasma gondii diphosphate + S-farnesyl protein
-
?
2.5.1.58 farnesyl diphosphate + protein-cysteine enzyme responsible for catalysing isoprene lipid modifications Toxoplasma gondii S-farnesyl protein + diphosphate
-
?

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.5.1.58 36
-
-
Toxoplasma gondii

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.5.1.58 8
-
-
Toxoplasma gondii

pH Range

EC Number pH Minimum pH Maximum Comment Organism
2.5.1.58 6 8.4 pH 6.0 and pH .4: about 80% of maximal activity, the enzyme activity is completely abolished at pH 4.0 Toxoplasma gondii

pH Stability

EC Number pH Stability pH Stability Maximum Comment Organism
2.5.1.58 4
-
the enzyme activity completely abolishes Toxoplasma gondii