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Literature summary for 2.1.1.100 extracted from

  • Anderson, J.L.; Henriksen, B.S.; Gibbs, R.A.; Hrycyna, C.A.
    The isoprenoid substrate specificity of isoprenylcysteine carboxylmethyltransferase: development of novel inhibitors (2005), J. Biol. Chem., 280, 29454-29461.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.100

Application

Application Comment Organism
medicine inhibition of the enzyme results in Ras mislocalization and loss of cellular transformation ability, making it an attractive and novel anticancer target Homo sapiens
medicine inhibition of the enzyme results in Ras mislocalization and loss of cellular transformation ability, making it an attractive and novel anticancer target Saccharomyces cerevisiae

Cloned(Commentary)

Cloned (Comment) Organism
His-Ste14p, which encodes Ste14p with a 10 x histidine tag followed by a triply iterated myc epitope repeat at the N terminus under the constitutive control of the phosphoglycerate kinase promoter, overexpressed in Saccharomyces cerevisiae Saccharomyces cerevisiae
into the pCHH10m3N vector, overexpressed in Saccharomyces cerevisiae Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine shows a mix of competitive and uncompetitive inhibition Homo sapiens
N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine shows a mix of competitive and uncompetitive inhibition Saccharomyces cerevisiae
N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine competitive inhibitor of overexpressed yeast Icmt Saccharomyces cerevisiae

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Homo sapiens 16020
-
membrane
-
 Saccharomyces cerevisiae 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Saccharomyces cerevisiae
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Saccharomyces cerevisiae

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine relatively good substrate for the human Icmt enzyme Homo sapiens S-adenosyl-L-homocysteine + N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine methyl ester
-
 ?
S-adenosyl-L-methionine + N-acetyl-S-farnesyl-L-cysteine isoprenoid moiety as a key substrate recognition element for Icmt Homo sapiens S-adenosyl-L-homocysteine + N-acetyl-S-farnesyl-L-cysteine methyl ester
-
 ?
S-adenosyl-L-methionine + N-acetyl-S-farnesyl-L-cysteine isoprenoid moiety as a key substrate recognition element for Icmt Saccharomyces cerevisiae S-adenosyl-L-homocysteine + N-acetyl-S-farnesyl-L-cysteine methyl ester
-
 ?

Synonyms

Synonyms Comment Organism
Icmt
-
 Homo sapiens
isoprenylcysteine carboxylmethyltransferase
-
 Homo sapiens
isoprenylcysteine carboxylmethyltransferase
-
 Saccharomyces cerevisiae
Ste14p
-
 Saccharomyces cerevisiae

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0171
-
 N-acetyl-S-(3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2Z,6E,10-trien-1-yl)-L-cysteine
-
 Saccharomyces cerevisiae
0.0354
-
 N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine competitive inhibition Saccharomyces cerevisiae
0.1193
-
 N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine competitive inhibition Homo sapiens
0.3772
-
 N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine uncompetitive inhibition Homo sapiens
0.6144
-
 N-Acetyl-S-(3-(3-methylbut-2-enyl)-5-(4-phenyl)phenylpent-2Z-en-1-yl)-L-cysteine uncompetitive inhibition Saccharomyces cerevisiae