ReviewKeynoteEmerging strategies of targeting lipoprotein lipase for metabolic and cardiovascular diseases

•Lipoprotein lipase plays a key part in human triglyceride metabolism.•Certain liver-derived proteins stimulate or inhibit LPL activity.•Novel small-molecule and gene therapy approaches directly stimulate LPL activity.•Antisense oligos, antibodies and siRNA against anti-LPL proteins stimulate LPL.

Although statins and other pharmacological approaches have improved the management of lipid abnormalities, there exists a need for newer treatment modalities especially for the management of hypertriglyceridemia. Lipoprotein lipase (LPL), by promoting hydrolytic cleavage of the triglyceride core of lipoproteins, is a crucial node in the management of plasma lipid levels. Although LPL expression and activity modulation is observed as a pleiotropic action of some the commonly used lipid lowering drugs, the deliberate development of drugs targeting LPL has not occurred yet. In this review, we present the biology of LPL, highlight the LPL modulation property of currently used drugs and review the novel emerging approaches to target LPL.