Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.5.1.58 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
Search for more literature for 2.5.1.58

Application

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

Inhibitors

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

Metals/Ions

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
farnesyl diphosphate + protein-cysteine Toxoplasma gondii enzyme responsible for catalysing isoprene lipid modifications S-farnesyl protein + diphosphate
-
 ?

Organism

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

Purification (Commentary)

Purification (Comment) Organism
-
 Toxoplasma gondii

Substrates and Products (Substrate)

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

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
-
 Toxoplasma gondii

pH Range

pH Minimum pH Maximum Comment Organism
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

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