Targeting PCSK9 for therapeutic gains
Related Experiment Video
Updated: Apr 17, 2026

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
Michael D Shapiro1, Sergio Fazio, Hagai Tavori
1The Knight Cardiovascular Institute, Center for Preventive Cardiology, Oregon Health and Science University, 3181 S.W. Sam Jackson Park Road, Portland, OR, USA.
Abstract:
Even though it is only a little over a decade from the discovery of proprotein convertase subtilisin/kexin type 9 (PCSK9) as a plasma protein that associates with both hypercholesterolemia and low cholesterol syndromes, a rich literature has developed describing its unique physiology and the impact of antagonism of this molecule on cholesterol metabolism for therapeutic purposes. Indeed, the PCSK9 story is unfolding rapidly, with many answers and more questions. This review summarizes the most recent data from phase II/III clinical trials of PCSK9 inhibition with the three leading antibodies, highlights the clinical significance of the ongoing studies, and suggests future areas of investigation based on recent basic science discoveries on the physiology of PCSK9.
Related Concept Videos
Pharmacogenomics: Identification of New Drug Targets
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Atherosclerosis III: Management
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Lipid-Lowering Drugs: Statins and Miscellaneous Agents

