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Updated: Jun 21, 2026

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
Recent patents on PCSK9: a new target for treating hypercholesterolemia
Hai Li1, Haixia Li, Nick Ziegler
1Department of VeteransAffairs, Palo Alto Health Care System (154P), Palo Alto, CA 94304, USA. haili_65@yahoo.com
Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates low-density lipoprotein cholesterol (LDL-c). Inhibiting PCSK9 offers a promising strategy for reducing LDL-c levels and managing hypercholesterolemia.
Area of Science:
- Biochemistry
- Genetics
- Pharmacology
Background:
- Proprotein convertase subtilisin/kexin type 9 (PCSK9) is crucial in regulating plasma low-density lipoprotein cholesterol (LDL-c).
- PCSK9 downregulates the low-density lipoprotein receptor (LDLR) in the liver, impacting LDL-c levels.
- Gain-of-function mutations in PCSK9 cause hypercholesterolemia, while loss-of-function mutations lead to hypocholesterolemia.
Purpose of the Study:
- To review current knowledge on PCSK9.
- To summarize recent patents on PCSK9 inhibition strategies for reducing plasma LDL-c.
Main Methods:
- Review of scientific literature and patent applications.
- Analysis of methods targeting PCSK9 expression or activity.
Main Results:
- PCSK9 inhibition is a viable therapeutic approach for lowering LDL-c.
- Various patented methods, including antisense oligonucleotides, siRNAs, antibodies, and small molecules, aim to reduce PCSK9 expression.
Conclusions:
- PCSK9 is a significant therapeutic target for managing hypercholesterolemia.
- Emerging patented technologies offer effective strategies for PCSK9 inhibition and LDL-c reduction.
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