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Figure 1 Overview of lipoprotein metabolism and effects of novel lipid-modulating approaches
Figure 1 | Overview of lipoprotein metabolism and effects of novel lipid-modulating approaches. The major role of lipoproteins is to deliver lipids to peripheral tissues and return lipids for excretion or recycling. Because elevated LDL-cholesterol (LDL-C) level is a major cardiovascular risk factor, several approaches have been developed to target LDL-C levels. The most recent LDL-C-lowering strategies being investigated (including monoclonal antibodies [mAbs] and vaccines against PCSK9) allow achievement of very low LDL-C levels. Within cells, compensatory mechanisms are activated to counteract the low levels of circulating cholesterol, allowing normal cell activity. Inhibition of cholesteryl ester transfer protein (CETP) leads to an increase in HDL-cholesterol levels; however, blocking the activity of this transfer protein also results in the reduction of apolipoprotein B (apoB)-containing lipoprotein levels, which might explain the reduction of cardiovascular events observed in anacetrapib-treated patients. CE, cholesteryl ester; CETPi, cholesteryl ester transfer protein inhibitors; IDL, intermediate-density lipoprotein; LDLR, low density lipoprotein receptor; LCAT, lecithin–cholesterol acyltransferase; LXR, liver X receptor; RXR, retinoid X receptors; SRB1, scavenger receptor class B type 1; SREBP, sterol regulatory element-binding protein; TG, triglycerides; VLDL, very low density lipoprotein. Catapano, A. L. (2018) Atherogenic lipoproteins as treatment targets Nat. Rev. Cardiol. doi: /nrcardio
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