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Literature summary for 3.4.99.B1 extracted from

  • Mohammed, I.; Hampton, S.E.; Ashall, L.; Hildebrandt, E.R.; Kutlik, R.A.; Manandhar, S.P.; Floyd, B.J.; Smith, H.E.; Dozier, J.K.; Distefano, M.D.; Schmidt, W.K.; Dore, T.M.
    8-Hydroxyquinoline-based inhibitors of the Rce1 protease disrupt Ras membrane localization in human cells (2016), Bioorg. Med. Chem., 24, 160-178 .
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
expression in Saccharomyces cerevisiae Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-(((1-hydroxynaphthalen-2-yl)(phenyl)methyl)amino)benzoic acid inhibitor causes a reduction in Rce1 in vitro activity, exhibits low cell toxicity, and induces mislocalization of EGFP-Ras from the plasma membrane in human colon carcinoma cells. FTase activity is not inhibited at concentrations as high as 50 microM Homo sapiens
4-(((4-bromo-2,6-difluorophenyl)(1-hydroxynaphthalen-2-yl)methyl)amino)benzoic acid inhibitor causes a reduction in Rce1 in vitro activity, exhibits low cell toxicity, and induces mislocalization of EGFP-Ras from the plasma membrane in human colon carcinoma cells. FTase activity is not inhibited at concentrations as high as 50 microM Homo sapiens
4-(((4-bromophenyl)(1-hydroxynaphthalen-2-yl)methyl)amino)benzoic acid inhibitor causes a reduction in Rce1 in vitro activity, exhibits low cell toxicity, and induces mislocalization of EGFP-Ras from the plasma membrane in human colon carcinoma cells. FTase activity is not inhibited at concentrations as high as 50 microM Homo sapiens
4-(((4-bromophenyl)(8-hydroxyquinolin-7-yl)methyl)amino)benzoate inhibitor causes a reduction in Rce1 in vitro activity, exhibits low cell toxicity, and induces mislocalization of EGFP-Ras from the plasma membrane in human colon carcinoma cells. FTase activity is not inhibited at concentrations as high as 50 microM Homo sapiens
4-(((8-hydroxyquinolin-7-yl)(phenyl)methyl)amino)benzoate inhibitor causes a reduction in Rce1 in vitro activity, exhibits low cell toxicity, and induces mislocalization of EGFP-Ras from the plasma membrane in human colon carcinoma cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y256
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HCT-116 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ABZ-KSKTKC(S-farnesyl)-K(Dnp)-IM + H2O
-
 Homo sapiens ?
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0067
-
 pH 7.0, 30°C Homo sapiens 4-(((4-bromophenyl)(8-hydroxyquinolin-7-yl)methyl)amino)benzoate
0.0069
-
 pH 7.0, 30°C Homo sapiens 4-(((8-hydroxyquinolin-7-yl)(phenyl)methyl)amino)benzoate