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Updated: Apr 4, 2026

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
[PCSK9 inhibitors. A new approach for treatment of hypercholesterolemia]
Abstract:
To date HMG-CoA-reductase inhibitors are the most effective drugs for reduction of LDL-cholesterol levels and for prevention of cardiovascular events. Inhibition of the enzyme PCSK9 (proprotein convertase subtilisin/kexin type 9), which is involved in depletion of the LDL-receptor, is a new pharmacologic approach. Inhibition of PCSK9 by monoclonal antibodies provokes an additional reduction of LDL-cholesterol levels by 50-60 % in addition to statins. Previous phase III studies indicate good compatibility. Ongoing long-term studies will answer questions of safety and influence on cardiovascular events. Although those results are not available yet, alirocumab and evolocumab have already been recommendd for approval.
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