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Literature summary for 2.3.1.26 extracted from

  • An, S.; Park, Y.; Paik, Y.; Jeong, T.; Lee, W.S.
    Human ACAT inhibitory effects of shikonin derivatives from Lithospermum erythrorhizon (2007), Bioorg. Med. Chem. Lett., 17, 1112-1116.
    View publication on PubMed
Search for more literature for 2.3.1.26

Application

Application Comment Organism
pharmacology ACAT-1 and ACAT-2 selective inhibitors may prove to have clinical benefit to reduce atherosclerosis via directly reducing the size of the lipid-rich core in the atherosclerotic plaques or the absorption of cholesterol in intestine, respectively Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
a stable cell line expressing hACAT-1 from AC-29 cells is established Homo sapiens
a stable cell line expressing hACAT-2 from AC-29 cells is established Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl (9Z,12E)-octadeca-9,12-dienoate
-
 Homo sapiens
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl 3-methylbutanoate
-
 Homo sapiens
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl benzoate
-
 Homo sapiens
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl butanoate
-
 Homo sapiens
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pent-4-enoate
-
 Homo sapiens
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pentanoate
-
 Homo sapiens
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl propanoate
-
 Homo sapiens
acetylshikonin
-
 Homo sapiens
beta-hydroxyisovalerylshikonin
-
 Homo sapiens
isobutyrylshikonin
-
 Homo sapiens
shikonin
-
 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
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
ACAT-1
-
 Homo sapiens
ACAT-2
-
 Homo sapiens
acyl-CoA:cholesterol acyltransferase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0138
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl 3-methylbutanoate
0.0224
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl propanoate
0.0251
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl 3-methylbutanoate
0.0287
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl propanoate
0.0307
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pent-4-enoate
0.0496
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl butanoate
0.0537
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl benzoate
0.0562
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl benzoate
0.0575
-
-
 Homo sapiens isobutyrylshikonin
0.0704
-
-
 Homo sapiens shikonin
0.0714
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pent-4-enoate
0.0776
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl butanoate
0.0845
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pentanoate
0.0948
-
-
 Homo sapiens (1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pentanoate
0.1122
-
-
 Homo sapiens acetylshikonin
0.1289
-
-
 Homo sapiens acetylshikonin
0.1382
-
-
 Homo sapiens shikonin
0.1698
-
-
 Homo sapiens beta-hydroxyisovalerylshikonin
0.1869
-
-
 Homo sapiens beta-hydroxyisovalerylshikonin