PCSK9: an emerging target for treatment of hypercholesterolemia (Q37825903)

23 August 2017

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title

PCSK9: an emerging target for treatment of hypercholesterolemia (English)

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23 August 2017

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2

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23 August 2017

Christopher J Duff

1

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PubMed ID

21204732

23 August 2017

language of work or name

English

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publication date

5 January 2011

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Expert Opinion on Therapeutic Targets

23 August 2017

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23 August 2017

15

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23 August 2017

2

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23 August 2017

157-168

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Familial hypercholesterolemia: defective binding of lipoproteins to cultured fibroblasts associated with impaired regulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase activity

23 August 2017

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Familial defective apolipoprotein B-100: low density lipoproteins with abnormal receptor binding

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Mutations in PCSK9 cause autosomal dominant hypercholesterolemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A third major locus for autosomal dominant hypercholesterolemia maps to 1p34.1-p32

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Strategies for proprotein convertase subtilisin kexin 9 modulation: a perspective on recent patents

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9 and LDL cholesterol: unravelling the target to design the bullet

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Molecular basis of PCSK9 function

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9: an enigmatic protease.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The unique role of proprotein convertase subtilisin/kexin 9 in cholesterol homeostasis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9 as a therapeutic target of dyslipidemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The secretory proprotein convertase neural apoptosis-regulated convertase 1 (NARC-1): liver regeneration and neuronal differentiation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Mammalian subtilisin/kexin isozyme SKI-1: A widely expressed proprotein convertase with a unique cleavage specificity and cellular localization

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Functional characterization of Narc 1, a novel proteinase related to proteinase K

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The activation and physiological functions of the proprotein convertases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

NARC-1/PCSK9 and its natural mutants: zymogen cleavage and effects on the low density lipoprotein (LDL) receptor and LDL cholesterol

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Structural and biophysical studies of PCSK9 and its mutants linked to familial hypercholesterolemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The self-inhibited structure of full-length PCSK9 at 1.9 A reveals structural homology with resistin within the C-terminal domain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The crystal structure of PCSK9: a regulator of plasma LDL-cholesterol

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Activation of the furin endoprotease is a multiple-step process: requirements for acidification and internal propeptide cleavage

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Proprotein convertase models based on the crystal structures of furin and kexin: explanation of their specificity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Combined analysis of oligonucleotide microarray data from transgenic and knockout mice identifies direct SREBP target genes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Novel putative SREBP and LXR target genes identified by microarray analysis in liver of cholesterol-fed mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Sterol-dependent regulation of proprotein convertase subtilisin/kexin type 9 expression by sterol-regulatory element binding protein-2.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Adenoviral-mediated expression of Pcsk9 in mice results in a low-density lipoprotein receptor knockout phenotype

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Post-transcriptional regulation of low density lipoprotein receptor protein by proprotein convertase subtilisin/kexin type 9a in mouse liver.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Decreased plasma cholesterol and hypersensitivity to statins in mice lacking Pcsk9

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Proprotein convertase subtilisin kexin 9: the third locus implicated in autosomal dominant hypercholesterolemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Effect of mutations in the PCSK9 gene on the cell surface LDL receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Effects of pH and low density lipoprotein (LDL) on PCSK9-dependent LDL receptor regulation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Secreted PCSK9 decreases the number of LDL receptors in hepatocytes and in livers of parabiotic mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Proprotein convertase subtilisin/kexin type 9 (PCSK9): hepatocyte-specific low-density lipoprotein receptor degradation and critical role in mouse liver regeneration

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Plasma PCSK9 preferentially reduces liver LDL receptors in mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Secreted proprotein convertase subtilisin/kexin type 9 reduces both hepatic and extrahepatic low-density lipoprotein receptors in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Mutations in the PCSK9 gene in Norwegian subjects with autosomal dominant hypercholesterolemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A mutation in PCSK9 causing autosomal-dominant hypercholesterolemia in a Utah pedigree

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Severe hypercholesterolemia in four British families with the D374Y mutation in the PCSK9 gene: long-term follow-up and treatment response

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Molecular characterization of loss-of-function mutations in PCSK9 and identification of a compound heterozygote

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9 dominant negative mutant results in increased LDL catabolic rate and familial hypobetalipoproteinemia.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Low LDL cholesterol in individuals of African descent resulting from frequent nonsense mutations in PCSK9.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The proprotein convertase (PC) PCSK9 is inactivated by furin and/or PC5/6A: functional consequences of natural mutations and post-translational modifications

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Missense mutations in the PCSK9 gene are associated with hypocholesterolemia and possibly increased response to statin therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Sequence variations in PCSK9, low LDL, and protection against coronary heart disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A PCSK9 missense variant associated with a reduced risk of early-onset myocardial infarction

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A spectrum of PCSK9 alleles contributes to plasma levels of low-density lipoprotein cholesterol.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The PCSK9 gene R46L variant is associated with lower plasma lipid levels and cardiovascular risk in healthy U.K. men.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Identification and characterization of two non-secreted PCSK9 mutants associated with familial hypercholesterolemia in cohorts from New Zealand and South Africa.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Antibody-mediated disruption of the interaction between PCSK9 and the low-density lipoprotein receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Binding of proprotein convertase subtilisin/kexin type 9 to epidermal growth factor-like repeat A of low density lipoprotein receptor decreases receptor recycling and increases degradation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Molecular basis for LDL receptor recognition by PCSK9

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Catalytic activity is not required for secreted PCSK9 to reduce low density lipoprotein receptors in HepG2 cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Structure of the LDL receptor extracellular domain at endosomal pH

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Acid-dependent ligand dissociation and recycling of LDL receptor mediated by growth factor homology region

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Structural requirements for PCSK9-mediated degradation of the low-density lipoprotein receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

LXR regulates cholesterol uptake through Idol-dependent ubiquitination of the LDL receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Annexin A2 is a C-terminal PCSK9-binding protein that regulates endogenous low density lipoprotein receptor levels

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A proprotein convertase subtilisin-like/kexin type 9 (PCSK9) C-terminal domain antibody antigen-binding fragment inhibits PCSK9 internalization and restores low density lipoprotein uptake

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The C679X mutation in PCSK9 is present and lowers blood cholesterol in a Southern African population

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Statins upregulate PCSK9, the gene encoding the proprotein convertase neural apoptosis-regulated convertase-1 implicated in familial hypercholesterolemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Antagonism of Secreted PCSK9 Increases Low Density Lipoprotein Receptor Expression in HepG2 Cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9 binds to multiple receptors and can be functionally inhibited by an EGF-A peptide.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A proprotein convertase subtilisin/kexin type 9 neutralizing antibody reduces serum cholesterol in mice and nonhuman primates

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A PCSK9-binding antibody that structurally mimics the EGF(A) domain of LDL-receptor reduces LDL cholesterol in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Antisense inhibition of proprotein convertase subtilisin/kexin type 9 reduces serum LDL in hyperlipidemic mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

A locked nucleic acid antisense oligonucleotide (LNA) silences PCSK9 and enhances LDLR expression in vitro and in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Therapeutic RNAi targeting PCSK9 acutely lowers plasma cholesterol in rodents and LDL cholesterol in nonhuman primates

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Berberine decreases PCSK9 expression in HepG2 cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Hepatocyte nuclear factor 1alpha plays a critical role in PCSK9 gene transcription and regulation by the natural hypocholesterolemic compound berberine

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Small-molecule inhibitors of protein-protein interactions: progressing towards the dream

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Binding of small molecules to an adaptive protein-protein interface

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein interactions

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Structural basis for LFA-1 inhibition upon lovastatin binding to the CD11a I-domain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Cellular and secreted pro-protein convertase subtilisin/kexin type 9 catalytic activity in hepatocytes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Genetic and metabolic determinants of plasma PCSK9 levels

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Degradation of the LDL receptors by PCSK9 is not mediated by a secreted protein acted upon by PCSK9 extracellularly

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Overexpression of PCSK9 accelerates the degradation of the LDLR in a post-endoplasmic reticulum compartment

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The cellular trafficking of the secretory proprotein convertase PCSK9 and its dependence on the LDLR

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Dissection of the endogenous cellular pathways of PCSK9-induced low density lipoprotein receptor degradation: evidence for an intracellular route

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Intrabodies: production and promise

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Mipomersen, an apolipoprotein B synthesis inhibitor, for lowering of LDL cholesterol concentrations in patients with homozygous familial hypercholesterolaemia: a randomised, double-blind, placebo-controlled trial

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

The proprotein convertase PCSK9 induces the degradation of low density lipoprotein receptor (LDLR) and its closest family members VLDLR and ApoER2

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9 is required for the disposal of non-acetylated intermediates of the nascent membrane protein BACE1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9 is not involved in the degradation of LDL receptors and BACE1 in the adult mouse brain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

Analysis of lipid pathway genes indicates association of sequence variation near SREBF1/TOM1L2/ATPAF2 with dementia risk

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

No genetic association between PCSK9 polymorphisms and Alzheimer's disease and plasma cholesterol level in Japanese patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9 impedes hepatitis C virus infection in vitro and modulates liver CD81 expression

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

PCSK9-deficient mice exhibit impaired glucose tolerance and pancreatic islet abnormalities.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2011.547480

10.1517/14728222.2011.547480

21 January 2018

Identifiers

DOI

1 reference

23 August 2017

1 reference

PubMed ID

21204732