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Literature summary 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

Application

EC Number Application Comment Organism
2.3.1.26 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)

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

Inhibitors

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

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 Mus musculus
-
 CoA + cholesterol ester
-
 ?
2.3.1.26 acyl-CoA + cholesterol Homo sapiens
-
 CoA + cholesterol ester
-
 ?
2.3.1.26 acyl-CoA + cholesterol Rattus norvegicus
-
 CoA + cholesterol ester
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.26 Homo sapiens
-
-
-
2.3.1.26 Mus musculus
-
-
-
2.3.1.26 Rattus norvegicus
-
-
-

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.26 37
-
 activity assay Homo sapiens
2.3.1.26 37
-
 activity assay Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.26 7.4
-
 activity assay Homo sapiens
2.3.1.26 7.4
-
 activity assay Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.26 0.002
-
 liver Rattus norvegicus pactimibe sulfate
2.3.1.26 0.0027
-
 macrophage Rattus norvegicus pactimibe sulfate
2.3.1.26 0.003
-
 ACAT-2 Homo sapiens pactimibe sulfate
2.3.1.26 0.0043
-
 macrophage Rattus norvegicus avasimibe
2.3.1.26 0.0047
-
 THP-1 cell Homo sapiens pactimibe sulfate
2.3.1.26 0.0049
-
 ACAT-1 Homo sapiens pactimibe sulfate
2.3.1.26 0.0082
-
 liver Rattus norvegicus avasimibe
2.3.1.26 0.0092
-
 ACAT-2 Homo sapiens avasimibe
2.3.1.26 0.014
-
 THP-1 cell Homo sapiens avasimibe
2.3.1.26 0.0235
-
 ACAT-1 Homo sapiens avasimibe