Large-scale epidemiological studies firmly established the association between low plasma levels of
high-density lipoprotein-cholesterol (HDL-C) and elevated risk of cardiovascular disease. This relationship is
thought to reflect the key biological function of HDL, which involves reverse cholesterol transport from the arterial
wall to the liver for further excretion from the body. Other aspects of the cardioprotective HDL functionality
include antioxidative, anti-inflammatory, anti-apoptotic, anti-thrombotic, vasodilatory, anti-infectious and antidiabetic
activities. Over the last decades, wide interest in HDL as an athero- and cardioprotective particle has
resulted in the development of HDL-C raising as a therapeutic approach to reduce cardiovascular risk. Several
strategies to increase circulating HDL-C concentrations were developed that primarily included use of niacin and
fibrates as potent HDL-C raising agents. In the statin era, inhibition of cholesteryl ester transfer protein, infusion
of artificially reconstituted HDL and administration of apolipoprotein A-I mimetics were established as novel
approaches to raise HDL-C. More recently, other strategies targeting HDL metabolism, such as upregulation of
apolipoprotein A-I production by the liver, were added to the list of HDL therapeutics. This review summarises
current knowledge of novel HDL-targeting therapies and discusses perspectives of their use.
Keywords: Atherosclerosis, apoA-I, cardiovascular disease, CETP, HDL, lipoprotein, miRNA, rHDL.
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