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Literature summary for 2.3.1.26 extracted from

  • Ohshiro, T.; Kobayashi, K.; Ohba, M.; Matsuda, D.; Rudel, L.L.; Takahashi, T.; Doi, T.; Tomoda, H.
    Selective inhibition of sterolO-acyltransferase 1 isozyme by beauveriolide III in intact cells (2017), Sci. Rep., 7, 4163 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression in CHO cell Homo sapiens
expression in CHO cell Chlorocebus aethiops

Inhibitors

Inhibitors Comment Organism Structure
beauveriolide I selectively inhibits isoform SOAT1 in a cell-based assay, and shows dual inhibition of SOAT1 and SOAT2 in the enzyme-based assay Chlorocebus aethiops
beauveriolide I selectively inhibits isoform SOAT1 in a cell-based assay, and shows dual inhibition of SOAT1 and SOAT2 in the enzyme-based assay Homo sapiens
beauveriolide III selectively inhibits isoform SOAT1 in a cell-based assay, and shows dual inhibition of SOAT1 and SOAT2 in the enzyme-based assay . Beauveriolide III binds to a putative active site responsible for SOAT1 that is located on the cytosolic side of the ER, while Beauveriolide III is not accessible to the corresponding active site for SOAT2 located on the luminal side Chlorocebus aethiops
beauveriolide III selectively inhibits isoform SOAT1 in a cell-based assay, and shows dual inhibition of SOAT1 and SOAT2 in the enzyme-based assay . Beauveriolide III binds to a putative active site responsible for SOAT1 that is located on the cytosolic side of the ER, while Beauveriolide III is not accessible to the corresponding active site for SOAT2 located on the luminal side Homo sapiens

Organism

Organism UniProt Comment Textmining
Chlorocebus aethiops O77760 isoform SOAT1
-
Homo sapiens P35610
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
oleoyl-CoA + cholesterol
-
Homo sapiens CoA + cholesterol oleate
-
?
oleoyl-CoA + cholesterol
-
Chlorocebus aethiops CoA + cholesterol oleate
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00051
-
cell-based assay, pH 7.2, 37°C Homo sapiens beauveriolide III
0.0006
-
cell-based assay, pH 7.2, 37°C Chlorocebus aethiops beauveriolide III
0.00061
-
cell-based assay, pH 7.2, 37°C Homo sapiens beauveriolide I
0.0009
-
cell-based assay, pH 7.2, 37°C Chlorocebus aethiops beauveriolide I
0.0012
-
enzyme-based assay, pH 7.2, 37°C Homo sapiens beauveriolide III
0.0012
-
enzyme-based assay, pH 7.2, 37°C Chlorocebus aethiops beauveriolide III
0.003
-
enzyme-based assay, pH 7.2, 37°C Chlorocebus aethiops beauveriolide I
0.0032
-
enzyme-based assay, pH 7.2, 37°C Homo sapiens beauveriolide I