Acyl-CoA:Cholesterol Acyltransferase

Supporting information

Acyl-coenzyme (CoA):cholesterol acyltransferases (ACATs), EC, are integral membrane proteins that belong to the membrane bound O-acyl transferase (MBOAT) family. Two ACAT isoforms have been identified to date, ACAT1 and ACAT2, both of which are important for cholesterol homeostasis in normal tissues.

ACATs are expressed at low levels in the membrane of the endoplasmic reticulum. ACAT1 has almost ubiquitous tissue expression, being expressed in macrophages, liver hepatocytes and neurons, amongst others. In contrast ACAT2 has a more limited expression profile, although it is also expressed in macrophages and hepatocytes, albeit at lower levels. ACATs catalyze the conversion of excess cholesterol to cholesteryl esters (CEs). Cholesterol itself determines the activity of ACAT1, with increases and reductions in cholesterol levels resulting in enhanced or suppressed ACAT1 activity, respectively. Certain factors can also regulate ACAT1 gene expression, for example interferon-γ, urotensin-II and dexamethasone enhance ACAT1 expression, whereas ACAT1 is downregulated by adiponectin.

The upregulation of ACAT1 expression and the chronic accumulation of CE is associated with the formation of foamy macrophages and the onset and progression of atherosclerosis. Therefore the ACATs have been identified as a potential antiatherosclerotic therapeutic target. Inhibition of ACAT has been shown to reduce atherosclerotic plaque CE content and cause plaque regression in vivo. Furthermore ACAT could be a potential target for the treatment of Alzheimer's disease (AD). ACAT inhibition reduced amyloid plaque density in a mouse model of AD, although the exact mechanism is yet to be determined.

To view external sources of pharmacological information for Acyl-CoA:Cholesterol Acyltransferase, please click here: IUPHAR Receptor Code

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
ACAT1 Human ACAT1 NM_000019 P24752
Mouse Acat1 NM_144784 Q8QZT1
Rat Acat1 NM_017075 NP_058771
ACAT2 Human ACAT2 NM_005891 Q9BWD1
Mouse Acat2 NM_009338 Q8CAY6
Rat Acat2 NM_001006995 Q5XI22

Literature for Acyl-CoA:Cholesterol Acyltransferase

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