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A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
08:14

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9

Published on: August 28, 2018

The promises of PCSK9 inhibition

Francine Petrides1, Kate Shearston, Mathias Chatelais

  • 1The University of New South Wales, Sydney, New South Wales, Australia.

Current Opinion in Lipidology
|July 3, 2013
PubMed
Abstract

Insights

Monoclonal antibodies targeting proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitors significantly lower LDL cholesterol. Recent clinical trials show PCSK9 inhibition is safe and effective for patients reaching cholesterol goals.

Area of Science:

  • Cardiovascular Medicine
  • Pharmacology
  • Genetics

Background:

  • Proprotein convertase subtilisin kexin type 9 (PCSK9) is a validated target for lowering LDL cholesterol.
  • PCSK9 acts as a secreted inhibitor of the LDL receptor.
  • Genetic regulation of PCSK9 by statins has been observed.

Purpose of the Study:

  • Review recent reports on PCSK9 inhibitors.
  • Summarize discovery and mode of action of PCSK9.
  • Focus on Phase I and II clinical trials of PCSK9 inhibitors.

Main Methods:

  • Literature review of 500 publications up to March 2013.
  • Analysis of Phase I and II clinical trial data from 2012.
  • Review of in-vivo studies on long-term PCSK9 inhibition.

Main Results:

  • Phase I and II trials in 2012 demonstrated significant LDL-C reduction with PCSK9 inhibitors.
  • Patients achieved target LDL-C goals with these therapies.
  • No severe or serious safety issues were reported in trials.

Conclusions:

  • PCSK9 inhibitors show promise in managing hypercholesterolemia.
  • Potential cardiovascular benefits of long-term PCSK9 inhibition warrant further investigation.
  • Potential side-effects of PCSK9 inhibition require discussion.

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