Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents - Volume 5, Issue 4, 2005

Reverse cholesterol transport (RCT) is one pathway for removing excessive cholesterol from extrahepatic cells and tissues and eventual transport to the liver for excretion thus reducing the accumulation of cholesterol in arteries. Activity of RCT is believed to be affected at least partially by the high density lipoprotein (HDL) concentration in the blood, since HDL is the major carrier of cellular cholesterol through RCT. This presum Read More

The concentration of HDL cholesterol is a powerful predictor of the occurrence of cardiovascular events, with a possible causal relationship between these variables. As such, the ability of pharmacological agents to influence HDL levels, and to affect the related processes such as reverse cholesterol transport, is of considerable relevance to the prevention and treatment of cardiovascular disease. Whilst currently available l Read More

High-density lipoproteins (HDLs) have several metabolic actions in vitro that are potentially anti-atherogenic. In addition to their role in reverse cholesterol transport, native HDLs have been shown to protect low-density lipoproteins (LDLs) against oxidative modification, to have anti-inflammatory properties, and to inhibit platelet aggregation. These actions have been shown to occur also in vivo in both experimental a Read More

Apolipoprotein A-I (apoA-I) is a 243 amino-acid cysteine deficient protein, containing 10 amphipathic domains, that allow its binding to a lipid-rich surface. It is the major protein component of high-density lipoproteins (HDL). Each HDL contains 2 or 3 copies of apoA-I plus various combinations of additional apolipoproteins (e.g. apoE, apoA-IV, apoA-II), lipid transport proteins (e.g. CETP and PLTP), and surface acting enzymes (e.g Read More

Apolipoprotein A-I (apoA-I) is the major protein in high density lipoprotein (HDL) and a major component of the reverse cholesterol transport pathway. ApoA-I also has been shown to have multiple anti-inflammatory properties including the ability to remove pro-inflammatory lipids, reduce monocyte chemotaxis and spreading, and alter interactions between T-cells and monocytes. A variant of apoA-I, apoA-IMilano, has been Read More

The atheroprotective effects of high density lipoprotein (HDL) have been established over the past several decades and this in turn has led to efforts to develop more effective and well-tolerated means for elevating this lipoprotein. The high levels of HDL associated with human deficiency of cholesteryl ester transfer protein (CETP) motivated the pharmaceutical industry to initiate programs throughout the 1990s aimed tow Read More

Because HDL is the best lipid biomarker of cardiovascular risk, much attention has been given to the effects of nutrients on the concentration and composition of HDL. Interpretation has sometimes been inappropriate since increments in HDL do not necessarily imply benefit and vice versa. In particular the strong genetic determinant of the HDL concentration and the heterogeneity of HDL composition need to be considered. C Read More