Background: One of the important factors in Low-Density Lipoprotein (LDL) metabolism
is the LDL receptor (LDLR) by its capacity to bind and subsequently clear cholesterol derived from
LDL (LDL-C) in the circulation. Proprotein Convertase Subtilisin-like Kexin type 9 (PCSK9) is a
newly discovered serine protease that destroys LDLR in the liver and thereby controls the levels of
LDL in plasma. Inhibition of PCSK9-mediated degradation of LDLR has, therefore, become a novel
target for lipid-lowering therapy.
Methods: We review the current understanding of the structure and function of PCSK9 as well as its
implications for the treatment of hyperlipidemia and atherosclerosis.
Results: New treatments such as monoclonal antibodies against PCSK9 may be useful agents to lower
plasma levels of LDL and hence prevent atherosclerosis.
Conclusion: PCSK9's mechanism of action is not yet fully clarified. However, treatments that target
PCSK9 have shown striking early efficacy and promise to improve the lives of countless patients with
hyperlipidemia and atherosclerosis.