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Literature summary extracted from

  • Zhan, Y.; Zhang, X.W.; Xiong, Y.; Li, B.L.; Nan, F.J.
    Design and synthesis of simple, yet potent and selective non-ring-A pyripyropene A-based inhibitors of acyl-coenzyme A: cholesterol acyltransferase 2 (ACAT2) (2015), Org. Biomol. Chem., 14, 747-751.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.3.1.26 drug development the enzyme is regarded as a potential therapeutic target for cardiovascular diseases Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.26 2-[(5aR,6R,8R,9aR,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
 Homo sapiens
2.3.1.26 2-[(5aR,6R,8R,9aR,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
 Homo sapiens
2.3.1.26 2-[(5aS,6S,8S,9aS)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
 Homo sapiens
2.3.1.26 2-[(5aS,6S,8S,9aS,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
 Homo sapiens
2.3.1.26 2-[(5aS,6S,8S,9aS,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
 Homo sapiens
2.3.1.26 additional information design and synthesis of simple, potent and selective non-ring-A pyripyropene A-based inhibitors of acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2), overview. Natural product pyripyropene A (PPPA) and its analogues are the only chemical type ACAT2-specific inhibitors and are isolated from the fungal strain Aspergillus fumigatus strain FO-12897 Homo sapiens
2.3.1.26 pyripyropene A
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.26 acyl-CoA + cholesterol Homo sapiens
-
 CoA + cholesterol ester
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.26 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.26 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.26 acyl-CoA + cholesterol
-
 Homo sapiens CoA + cholesterol ester
-
 ?
2.3.1.26 additional information NBD22-steryl ester fluorescence assay Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.26 ACAT2
-
 Homo sapiens
2.3.1.26 cholesterol acyltransferase 2
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.26 0.000077
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aR,6R,8R,9aR,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.000155
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aS,6S,8S,9aS)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.000185
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens pyripyropene A
2.3.1.26 0.000416
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aR,6R,8R,9aR,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.000743
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aS,6S,8S,9aS,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.001272
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aS,6S,8S,9aS,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.0017
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aR,6R,8R,9aR,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.001789
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aS,6S,8S,9aS,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.002456
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aR,6R,8R,9aR,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
2.3.1.26 0.003059
-
 isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens 2-[(5aS,6S,8S,9aS,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate

General Information

EC Number General Information Comment Organism
2.3.1.26 physiological function isozyme ACAT2 is responsible for absorption of dietary cholesterol from the intestine and lipoprotein production by the liver, the steryl esters catalyzed by ACAT2 can incorporate into both intracellular lipid droplets and extracellular lipoproteins Homo sapiens