Clinical aspects of PCSK9

Abstract Proprotein convertase subtilisin kexin type 9 (PCSK9) is a circulating protein that impairs LDL clearance by promoting the LDL receptor (LDLR) degradation. PCSK9 has emerged as a new pharmacological target for hypercholesterolemia, and different PCSK9 inhibitors are now evaluated in clinica...

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Published inAtherosclerosis Vol. 216; no. 2; pp. 258 - 265
Main Authors Cariou, Bertrand, Le May, Cédric, Costet, Philippe
Format Journal Article
LanguageEnglish
Published Amsterdam Elsevier Ireland Ltd 01.06.2011
Elsevier
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Abstract Abstract Proprotein convertase subtilisin kexin type 9 (PCSK9) is a circulating protein that impairs LDL clearance by promoting the LDL receptor (LDLR) degradation. PCSK9 has emerged as a new pharmacological target for hypercholesterolemia, and different PCSK9 inhibitors are now evaluated in clinical trials. Here, we propose an overview of the clinical perspectives of PCSK9. First, we describe the clinical features of patients with PCSK9 mutations, and how these variations impact the cardiovascular risk. Then, we extensively discuss the potential role of circulating PCSK9 as a new biomarker of lipid metabolism. Indeed, many studies conducted in healthy and type 2 diabetic patients have tested the association of circulating PCSK9 with LDL-cholesterol as well as with multiple metabolic parameters. The overall picture of the clinical relevance of circulating PCSK9 is complicated by the effect of nutritional status and hypolipidemic drugs such as statins, fibrates, ezetimibe on plasma PCSK9 concentrations. Finally, we present a brief overview of the available therapeutic strategies to inhibit PCSK9.
AbstractList Abstract Proprotein convertase subtilisin kexin type 9 (PCSK9) is a circulating protein that impairs LDL clearance by promoting the LDL receptor (LDLR) degradation. PCSK9 has emerged as a new pharmacological target for hypercholesterolemia, and different PCSK9 inhibitors are now evaluated in clinical trials. Here, we propose an overview of the clinical perspectives of PCSK9. First, we describe the clinical features of patients with PCSK9 mutations, and how these variations impact the cardiovascular risk. Then, we extensively discuss the potential role of circulating PCSK9 as a new biomarker of lipid metabolism. Indeed, many studies conducted in healthy and type 2 diabetic patients have tested the association of circulating PCSK9 with LDL-cholesterol as well as with multiple metabolic parameters. The overall picture of the clinical relevance of circulating PCSK9 is complicated by the effect of nutritional status and hypolipidemic drugs such as statins, fibrates, ezetimibe on plasma PCSK9 concentrations. Finally, we present a brief overview of the available therapeutic strategies to inhibit PCSK9.
Proprotein convertase subtilisin kexin type 9 (PCSK9) is a circulating protein that impairs LDL clearance by promoting the LDL receptor (LDLR) degradation. PCSK9 has emerged as a new pharmacological target for hypercholesterolemia, and different PCSK9 inhibitors are now evaluated in clinical trials. Here, we propose an overview of the clinical perspectives of PCSK9. First, we describe the clinical features of patients with PCSK9 mutations, and how these variations impact the cardiovascular risk. Then, we extensively discuss the potential role of circulating PCSK9 as a new biomarker of lipid metabolism. Indeed, many studies conducted in healthy and type 2 diabetic patients have tested the association of circulating PCSK9 with LDL-cholesterol as well as with multiple metabolic parameters. The overall picture of the clinical relevance of circulating PCSK9 is complicated by the effect of nutritional status and hypolipidemic drugs such as statins, fibrates, ezetimibe on plasma PCSK9 concentrations. Finally, we present a brief overview of the available therapeutic strategies to inhibit PCSK9.
Author Costet, Philippe
Le May, Cédric
Cariou, Bertrand
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Issue 2
Keywords PCSK9
Hypercholesterolemia
Lipoprotein
Statin
LDL
Metabolic diseases
Lipids
Cardiovascular disease
Hyperlipoproteinemia
Statin derivative
Cholesterol
Vascular disease
Lipoprotein LDL
Atherosclerosis
Dyslipemia
Antilipemic agent
Language English
License CC BY 4.0
Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.
Distributed under a Creative Commons Attribution 4.0 International License: http://creativecommons.org/licenses/by/4.0
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PublicationTitle Atherosclerosis
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Snippet Abstract Proprotein convertase subtilisin kexin type 9 (PCSK9) is a circulating protein that impairs LDL clearance by promoting the LDL receptor (LDLR)...
Proprotein convertase subtilisin kexin type 9 (PCSK9) is a circulating protein that impairs LDL clearance by promoting the LDL receptor (LDLR) degradation....
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SubjectTerms Adolescent
Animals
Atherosclerosis (general aspects, experimental research)
Azetidines - therapeutic use
Biological and medical sciences
Blood and lymphatic vessels
Cardiology and cardiovascular system
Cardiology. Vascular system
Cardiovascular
Clinical trial. Drug monitoring
Diabetes Mellitus, Type 2 - blood
Endocrinology and metabolism
Ezetimibe
Female
Fibric Acids - therapeutic use
General pharmacology
Genes, Dominant
Human health and pathology
Humans
Hypercholesterolemia
Hypercholesterolemia - blood
Hépatology and Gastroenterology
LDL
Life Sciences
Lipid Metabolism
Lipoprotein
Male
Medical sciences
Mice
Mutation
Nutritional Status
PCSK9
Pharmacology. Drug treatments
Phenotype
Proprotein Convertase 9
Proprotein Convertases
Protease Inhibitors - pharmacology
Receptors, LDL - metabolism
Serine Endopeptidases - blood
Statin
Tissues and Organs
Title Clinical aspects of PCSK9
URI https://www.clinicalkey.es/playcontent/1-s2.0-S0021915011003601
https://dx.doi.org/10.1016/j.atherosclerosis.2011.04.018
https://www.ncbi.nlm.nih.gov/pubmed/21596380
https://search.proquest.com/docview/871003109
https://hal.science/hal-03013330
Volume 216
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