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Literature summary for 2.3.1.26 extracted from

  • Terasaka, N.; Miyazaki, A.; Kasanuki, N.; Ito, K.; Ubukata, N.; Koieyama, T.; Kitayama, K.; Tanimoto, T.; Maeda, N.; Inaba, T.
    ACAT inhibitor pactimibe sulfate (CS-505) reduces and stabilizes atherosclerotic lesions by cholesterol-lowering and direct effects in apolipoprotein E-deficient mice (2007), Atherosclerosis, 190, 239-247.
    View publication on PubMed
Search for more literature for 2.3.1.26

Application

Application Comment Organism
pharmacology the results strongly support the idea that CS-505 could be promising as a therapeutic agent for the treatment of atherosclerosis Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
a recombinant baculovirus transfer vector is constructed by subcloning of human ACAT-1 cDNA into pFASTBacHis Homo sapiens
a recombinant baculovirus transfer vector is constructed by subcloning of human ACAT-2 cDNA into pFASTBacHis Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
avasimibe CI-1011 Homo sapiens
avasimibe CI-1011 Mus musculus
avasimibe CI-1011 Rattus norvegicus
cholestyramine
-
 Homo sapiens
cholestyramine
-
 Mus musculus
cholestyramine
-
 Rattus norvegicus
pactimibe sulfate CS-505 Homo sapiens
pactimibe sulfate CS-505 Mus musculus
pactimibe sulfate CS-505 Rattus norvegicus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
microsomal fractions are prepared Homo sapiens
microsomal fractions are prepared Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Rattus norvegicus
-
peritoneal macrophage
-
 Rattus norvegicus
-
THP-1 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acyl-CoA + cholesterol
-
 Mus musculus CoA + cholesterol ester
-
 ?
acyl-CoA + cholesterol
-
 Homo sapiens CoA + cholesterol ester
-
 ?
acyl-CoA + cholesterol
-
 Rattus norvegicus CoA + cholesterol ester
-
 ?
oleoyl-CoA + cholesterol activity assay Homo sapiens CoA + cholesteryl oleate
-
 ?
oleoyl-CoA + cholesterol activity assay Homo sapiens ?
-
 ?
oleoyl-CoA + cholesterol activity assay Rattus norvegicus ?
-
 ?

Synonyms

Synonyms Comment Organism
ACAT
-
 Mus musculus
ACAT
-
 Rattus norvegicus
ACAT-1
-
 Homo sapiens
ACAT-2
-
 Homo sapiens
acyl-CoA:cholesterol acyltransferase
-
 Mus musculus
acyl-CoA:cholesterol acyltransferase
-
 Homo sapiens
acyl-CoA:cholesterol acyltransferase
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 activity assay Homo sapiens
37
-
 activity assay Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 activity assay Homo sapiens
7.4
-
 activity assay Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.002
-
 liver Rattus norvegicus pactimibe sulfate
0.0027
-
 macrophage Rattus norvegicus pactimibe sulfate
0.003
-
 ACAT-2 Homo sapiens pactimibe sulfate
0.0043
-
 macrophage Rattus norvegicus avasimibe
0.0047
-
 THP-1 cell Homo sapiens pactimibe sulfate
0.0049
-
 ACAT-1 Homo sapiens pactimibe sulfate
0.0082
-
 liver Rattus norvegicus avasimibe
0.0092
-
 ACAT-2 Homo sapiens avasimibe
0.014
-
 THP-1 cell Homo sapiens avasimibe
0.0235
-
 ACAT-1 Homo sapiens avasimibe