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Updated: Apr 18, 2026
08:14
A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
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PCSK9 inhibition: current concepts and lessons from human genetics
Fatima Rodriguez1, Joshua W Knowles
1Division of Cardiovascular Medicine, Stanford University, 300 Pasteur Dr, Stanford, CA, 94305, USA.
Current Atherosclerosis Reports
|February 1, 2015
Summary
Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibition effectively lowers low-density lipoprotein cholesterol (LDL-C) by 40-70%. This offers a vital alternative or supplement for patients intolerant to statins, aiding atherosclerotic cardiovascular disease (ASCVD) prevention.
Area of Science:
- Cardiovascular Medicine
- Biochemistry
- Pharmacology
Background:
- Low-density lipoprotein cholesterol (LDL-C) is key in atherosclerotic cardiovascular disease (ASCVD) pathogenesis.
- Statins are primary treatments, but some patients have intolerance or suboptimal response.
- Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates LDL receptor levels, impacting LDL-C.
Purpose of the Study:
- To review the role of PCSK9 inhibition in LDL-C reduction.
- To discuss PCSK9 inhibition as an alternative or supplement to statin therapy.
- To highlight the efficacy and tolerability of PCSK9 inhibitors in diverse patient groups.
Main Methods:
- Review of numerous phase II and III randomized controlled trials.
- Analysis of genetic studies on PCSK9 function and human disease.
- Evaluation of monoclonal antibodies targeting PCSK9.
Main Results:
- PCSK9 inhibition effectively lowers LDL-C by an additional 40-70%.
- Monoclonal antibodies against PCSK9 demonstrate good tolerability.
- Genetic evidence confirms PCSK9's critical role in lipid metabolism and ASCVD risk.
Conclusions:
- PCSK9 inhibition is a promising strategy for managing elevated LDL-C.
- It provides a valuable option for patients unresponsive or intolerant to statins.
- This approach supports ASCVD prevention across various patient populations.
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