APOC (Apolipoprotein C)阻害剤

The Apolipoprotein C (APOC) family, comprising APOC1, APOC2, APOC3, and APOC4, plays a critical role in lipid metabolism. These proteins are primarily associated with lipoprotein particles in the blood, such as high-density lipoproteins (HDL) and very low-density lipoproteins (VLDL). APOC proteins function in modulating lipoprotein metabolism and lipid transport; for example, APOC2 acts as an essential cofactor for lipoprotein lipase (LPL), an enzyme crucial for the hydrolysis of triglycerides. APOC3, on the other hand, inhibits LPL activity and also interferes with the uptake of triglyceride-rich lipoproteins by the liver. The balance in the activities of these apolipoproteins is vital for maintaining normal plasma lipid levels, and dysregulation can lead to lipid disorders, such as hypertriglyceridemia.

Targeting APOC (Apolipoprotein C) for disruption or inhibition is an area of interest, especially in the context of lipid disorders. Inhibiting APOC3 has garnered attention because of its role in inhibiting lipoprotein lipase and hepatic uptake of triglyceride-rich lipoproteins, factors contributing to elevated blood triglyceride levels. Small molecule inhibitors, antisense oligonucleotides, or RNA interference (RNAi) therapies can be used to decrease APOC3 levels, potentially improving lipid profiles.