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Literature summary for 2.3.1.26 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

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

Inhibitors

Inhibitors Comment Organism Structure
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-[(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-[(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-[(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-[(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
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
pyripyropene A
-
Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
ACAT2
-
Homo sapiens
cholesterol acyltransferase 2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
0.000185
-
isozyme ACAT2, pH and temperature not specified in the publication Homo sapiens pyripyropene A
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
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
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
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
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
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
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

General Information Comment Organism
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