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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

8.6K

Key aspects of PCSK9 inhibition beyond LDL lowering

Stéphane Ramin-Mangata, Valentin Blanchard, Gilles Lambert

    Current Opinion in Lipidology
    |September 11, 2018
    PubMed
    Abstract

    Insights

    Recent reviews explore proprotein convertase subtilisin/kexin type 9 (PCSK9) biology and its inhibitors. Key areas include lipoprotein (a) regulation and potential diabetes risks, with ongoing research into mechanisms.

    Area of Science:

    • Biochemistry
    • Cardiovascular Medicine
    • Pharmacology

    Background:

    • Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a critical role in regulating low-density lipoprotein receptor (LDLR) abundance.
    • PCSK9 influences lipid metabolism through distinct intracellular and extracellular pathways affecting LDLR degradation.

    Purpose of the Study:

    • To review current knowledge on PCSK9 biology and inhibition.
    • To examine PCSK9 inhibitors' effects on lipoprotein (a) levels.
    • To assess the potential diabetogenic effects of PCSK9 inhibition.

    Main Methods:

    • Literature review of recent findings on PCSK9 biology.
    • Analysis of studies on PCSK9 inhibitors' impact on lipoprotein (a).
    • Evaluation of clinical trial and experimental data regarding PCSK9 inhibition and diabetes risk.

    Main Results:

    • Two pathways for PCSK9-mediated LDLR degradation (extracellular and intracellular) are established.
    • Mechanisms by which PCSK9 inhibitors lower lipoprotein (a) remain debated.
    • Clinical trials have not shown an increased diabetes risk with PCSK9 inhibition, contrary to genetic predictions.

    Conclusions:

    • Further research is needed to fully elucidate PCSK9 trafficking pathways and LDLR degradation.
    • Additional studies are required to clarify the mechanisms of PCSK9 inhibition on lipoprotein (a) levels.
    • The precise role of PCSK9 in glucose metabolism warrants in-depth investigation.

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