Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Single Domain Antibodies Are Potent Inhibitors of Low Density Lipoprotein Receptor Degradation

New Therapies in the Treatment of High Cholesterol

(2015) William H. Shrank et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Amyloid Precursor-like Protein 2 and Sortilin Do Not Regulate the PCSK9 Convertase-mediated Low Density Lipoprotein Receptor Degradation but Interact with Each Other

(2015) Chutikarn Butkinaree et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PCSK9 deficiency unmasks a sex- and tissue-specific subcellular distribution of the LDL and VLDL receptors in mice

(2015) Anna Roubtsova et al.   JOURNAL OF LIPID RESEARCH

A cholesterol-lowering VLP vaccine that targets PCSK9

(2015) Erin Crossey et al.   VACCINE

GRP94 Regulates Circulating Cholesterol Levels through Blockade of PCSK9-Induced LDLR Degradation

(2015) Steve Poirier et al.   Cell Reports

Proprotein Convertase Subtilisin/Kexin Type 9 Deficiency Reduces Melanoma Metastasis in Liver

(2015) Xiaowei Sun et al.   NEOPLASIA

Reduction of Low-Density Lipoprotein Cholesterol by Monoclonal Antibody Inhibition of PCSK9

(2014) Evan A. Stein et al.   Annual Review of Medicine

PCSK9

(2014) Nabil G. Seidah et al.   CIRCULATION RESEARCH

Annexin A2 Reduces PCSK9 Protein Levels via a Translational Mechanism and Interacts with the M1 and M2 Domains of PCSK9

(2014) Kévin Ly et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Low Density Lipoprotein Receptor Class A Repeats AreO-Glycosylated in Linker Regions

(2014) Nis Borbye Pedersen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Peptide-Based Anti-PCSK9 Vaccines - An Approach for Long-Term LDLc Management

(2014) Gergana Galabova et al.   PLoS One

Bridging Lipid Metabolism and Innate Host Defense

(2014) C. dos Santos et al.   Science Translational Medicine

Nanobodies: Natural Single-Domain Antibodies

(2013) Serge Muyldermans   Annual Review of Biochemistry

Anti-Rotavirus Protein Reduces Stool Output in Infants With Diarrhea: A Randomized Placebo-Controlled Trial

(2013) Shafiqul A. Sarker et al.   GASTROENTEROLOGY

An Antibody against the C-Terminal Domain of PCSK9 Lowers LDL Cholesterol Levels In Vivo

(2013) Felix Schiele et al.   JOURNAL OF MOLECULAR BIOLOGY

Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Can Mediate Degradation of the Low Density Lipoprotein Receptor-Related Protein 1 (LRP-1)

(2013) Maryssa Canuel et al.   PLoS One

Novel Antiplatelet Agents: ALX-0081, a Nanobody Directed towards von Willebrand Factor

(2013) Jozef Bartunek et al.   Journal of Cardiovascular Translational Research

Gene Inactivation of Proprotein Convertase Subtilisin/Kexin Type 9 Reduces Atherosclerosis in Mice

(2012) Maxime Denis et al.   CIRCULATION

The M2 Module of the Cys-His-rich Domain (CHRD) of PCSK9 Protein Is Needed for the Extracellular Low-density Lipoprotein Receptor (LDLR) Degradation Pathway

(2012) Yascara Grisel Luna Saavedra et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Loss- and Gain-of-function PCSK9 Variants

(2012) Suzanne Benjannet et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Calcium-Independent Inhibition of PCSK9 by Affinity-Improved Variants of the LDL Receptor EGF(A) Domain

(2012) Yingnan Zhang et al.   JOURNAL OF MOLECULAR BIOLOGY

The biology and therapeutic targeting of the proprotein convertases

(2012) Nabil G. Seidah et al.   NATURE REVIEWS DRUG DISCOVERY

Exploring the interaction between SNP genotype and postmenopausal hormone therapy effects on stroke risk

(2012) Ying Huang et al.   Genome Medicine

Cholesterol-lowering Action of BNA-based Antisense Oligonucleotides Targeting PCSK9 in Atherogenic Diet-induced Hypercholesterolemic Mice

(2012) Tsuyoshi Yamamoto et al.   Molecular Therapy-Nucleic Acids

Circulating Proprotein Convertase Subtilisin/Kexin 9 (PCSK9) Regulates VLDLR Protein and Triglyceride Accumulation in Visceral Adipose Tissue

(2011) Anna Roubtsova et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

2009 Canadian Cardiovascular Society/Canadian guidelines for the diagnosis and treatment of dyslipidemia and prevention of cardiovascular disease in the adult – 2009 recommendations

(2011) Jacques Genest et al.   CANADIAN JOURNAL OF CARDIOLOGY

Mechanistic implications for LDL receptor degradation from the PCSK9/LDLR structure at neutral pH

(2011) Paola Lo Surdo et al.   EMBO REPORTS

Neutralization ofClostridium difficileToxin A with Single-domain Antibodies Targeting the Cell Receptor Binding Domain

(2011) Greg Hussack et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Clinical impact of serum proteins on drug delivery

(2011) Felix Kratz et al.   JOURNAL OF CONTROLLED RELEASE

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

(2010) Yan G. Ni et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

In VivoEvidence That Furin from Hepatocytes Inactivates PCSK9

(2010) Rachid Essalmani et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Effects of the Prosegment and pH on the Activity of PCSK9

(2010) Suzanne Benjannet et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2010) Yan G. Ni et al.   JOURNAL OF LIPID RESEARCH

Effects of PCSK9 genetic variants on plasma LDL cholesterol levels and risk of premature myocardial infarction in the Italian population

(2010) Ilaria Guella et al.   JOURNAL OF LIPID RESEARCH

Efficacy and safety of more intensive lowering of LDL cholesterol: a meta-analysis of data from 170 000 participants in 26 randomised trials

(2010)   LANCET

A Locked Nucleic Acid Antisense Oligonucleotide (LNA) Silences PCSK9 and Enhances LDLR Expression In Vitro and In Vivo

(2010) Nidhi Gupta et al.   PLoS One

Dissection of the Endogenous Cellular Pathways of PCSK9-induced Low Density Lipoprotein Receptor Degradation

(2009) Steve Poirier et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mechanism of LDL binding and release probed by structure-based mutagenesis of the LDL receptor

(2009) Sha Huang et al.   JOURNAL OF LIPID RESEARCH

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

(2009) J. C. Y. Chan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2008) LiXin Shan et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

PCSK9 as a therapeutic target of dyslipidemia

(2008) Nabil G Seidah   EXPERT OPINION ON THERAPEUTIC TARGETS

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

(2008) Ahmed Zaid et al.   HEPATOLOGY

General Strategy to Humanize a Camelid Single-domain Antibody and Identification of a Universal Humanized Nanobody Scaffold

(2008) Cécile Vincke et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2008) D.-W. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2008) M. Frank-Kamenetsky et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA