Introduction
Acyl-Coenzyme A Cholesterol Acyltransferase (ACAT), or also known as Sterol O-Acyltransferase (SOAT), is an important enzyme in the body.
Cholesterol esters were discovered in arterial lesions in 1910. Between 1980-1995, the interest in ACAT inhibitors grew, but some of the compounds looked at exhibited toxicity. In 1993, an ACAT gene was successfully cloned. This discovery led to more studies with ACAT and atherosclerosis.
[1]
add more history
Figure 1. ACAT as a Dimer of Dimers
Function
ACAT is an important enzyme that catalyzes the esterification of cholesterol to form cholesterol esters.
SOAT article [2]
ACAT article [3]
Disease
atherosclerosis, Alzheimer's Disease
Structural highlights
ACAT is a dimer of dimers, which is also known as a tetramer.
This
is about 260 kDa and is composed completely of helices, with each monomer containing 9 transmembrane helices.
The
was found to be the active arrangement.
The
is mobile and mostly hydrophobic.
Relevance
talk about inhibitor CI-976
Figure 2. CI-976 Inhibitor
