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Reverse cholesterol transport is a multi-step process resulting in the net movement of cholesterol from peripheral tissues back to the liver first via entering the lymphatic system, then the bloodstream. [1] Cholesterol from non-hepatic peripheral tissues is transferred to HDL by the ABCA1 (ATP-binding cassette transporter). [2]
Factors that act upon the ABCA1 transporter's expression or its posttranslational modification are also molecules that are involved in its subsequent function like fatty acids, cholesterol and also cytokines and cAMP. [14] Adiponectin induces reverse cholesterol transport by an ABCA1-dependent pathway. [15]
Several steps in the metabolism of HDL can participate in the transport of cholesterol from lipid-laden macrophages of atherosclerotic arteries, termed foam cells, to the liver for secretion into the bile. This pathway has been termed reverse cholesterol transport and is considered as the classical protective function of HDL toward atherosclerosis.
Atherosclerosis [a] is a pattern of the disease arteriosclerosis, [8] characterized by development of abnormalities called lesions in walls of arteries. This is a chronic inflammatory disease involving many different cell types and driven by elevated levels of cholesterol in the blood. [9]
This movement of cholesterol is known as reverse cholesterol transport and is a protective mechanism against the development of atherosclerosis, which is the principal cause of heart disease and stroke. SR-BI is crucial in carotenoid and vitamin E uptake in the small intestine.
Drugs in this class substantially increase HDL cholesterol, lower LDL cholesterol, and enhance reverse cholesterol transport. [citation needed]CETP inhibitors inhibit cholesterylester transfer protein (CETP), which normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL).
Mechanism of action of CER-001. CER-001 is designed to mimic the natural structure and function of nascent HDL, also known as pre-beta HDL. [12] This mimicry stimulates cholesterol efflux from macrophages, captures cholesterol and eliminates it via reverse lipid transport (RLT) pathway, also known as reverse cholesterol transport (RCT) pathway.
Cholesterol is biosynthesized by all animal cells [citation needed] and is an essential structural and signaling component of animal cell membranes. In vertebrates, hepatic cells typically produce the greatest amounts. In the brain, astrocytes produce cholesterol and transport it to neurons. [5]
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