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Literature summary extracted from

  • Ohshiro, T.; Ohte, S.; Matsuda, D.; Ohtawa, M.; Nagamitsu, T.; Sunazuka, T.; Harigaya, Y.; Rudel, L.L.; Omura, S.; Tomoda, H.
    Selectivity of pyripyropene derivatives in inhibition toward acyl-CoA:cholesterol acyltransferase 2 isozyme (2008), J. Antibiot., 61, 503-508.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.26 expression of isoforms ACAT1 and ACAT2 in CHO cells Chlorocebus aethiops

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.26 (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-6-(pentanoyloxy)-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-3-yl benzoate selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl dipentanoate selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl 3-methylbutanoate selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl diacetate i.e. pyripyropene A,selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-3-(butanoyloxy)-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl hexanoate selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (3S,4S,4aR,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-4,12,12b-trihydroxy-6a-methyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl (2E)-pent-2-enoate selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(1-methylethyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(2-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate selective for isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(4-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate selective for isoform ACAT2 Chlorocebus aethiops

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.26 Chlorocebus aethiops O77759 isoform ACAT2
-
2.3.1.26 Chlorocebus aethiops O77760 isoform ACAT1
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.26 0.000006
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl 3-methylbutanoate
2.3.1.26 0.00001
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl dipentanoate
2.3.1.26 0.00001
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (3S,4S,4aR,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-4,12,12b-trihydroxy-6a-methyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl (2E)-pent-2-enoate
2.3.1.26 0.00001
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(4-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
2.3.1.26 0.00001
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(2-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
2.3.1.26 0.00001
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(1-methylethyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
2.3.1.26 0.000012
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-3-(butanoyloxy)-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl hexanoate
2.3.1.26 0.000025
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-6-(pentanoyloxy)-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-3-yl benzoate
2.3.1.26 0.000062
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-6-(pentanoyloxy)-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-3-yl benzoate
2.3.1.26 0.00007
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl diacetate
2.3.1.26 0.00007
-
 isoform ACAT2, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl dipentanoate
2.3.1.26 0.0007
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(1-methylethyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
2.3.1.26 0.0028
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-3-(butanoyloxy)-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl hexanoate
2.3.1.26 0.0032
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(2-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
2.3.1.26 0.0035
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl 3-methylbutanoate
2.3.1.26 0.0038
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(4-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
2.3.1.26 0.0042
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (3S,4S,4aR,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-4,12,12b-trihydroxy-6a-methyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl (2E)-pent-2-enoate
2.3.1.26 0.08
-
 isoform ACAT1, cell-based assay Chlorocebus aethiops (3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl diacetate