The biology and therapeutic targeting of the proprotein convertases

A Small-Molecule Furin Inhibitor Inhibits Cancer Cell Motility and Invasiveness

(2015) Julia M. Coppola et al.   NEOPLASIA

Proprotein Convertase Inhibition Results in Decreased Ski Proliferation, Tumorigenesis, and Metastasis

(2015) Daniel E. Bassi et al.   NEOPLASIA

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

(2012) Maxime Denis et al.   CIRCULATION

SKI-1 and Furin Generate Multiple RGMa Fragments that Regulate Axonal Growth

(2012) Nardos G. Tassew et al.   DEVELOPMENTAL CELL

An Anti-PCSK9 Antibody Reduces LDL-Cholesterol On Top Of A Statin And Suppresses Hepatocyte SREBP-Regulated Genes

(2012) Liwen Zhang et al.   International Journal of Biological Sciences

Internalization of Proprotein Convertase PC7 from Plasma Membrane Is Mediated by a Novel Motif

(2012) Jeroen Declercq et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PCSK9 antibody reduces LDL cholesterol

(2012) Sarah Crunkhorn   NATURE REVIEWS DRUG DISCOVERY

Effect of a Monoclonal Antibody to PCSK9 on LDL Cholesterol

(2012) Evan A. Stein et al.   NEW ENGLAND JOURNAL OF MEDICINE

Human Subtilase SKI-1/S1P Is a Master Regulator of the HCV Lifecycle and a Potential Host Cell Target for Developing Indirect-Acting Antiviral Agents

(2012) Andrea D. Olmstead et al.   PLoS Pathogens

What lies ahead for the proprotein convertases?

(2011) Nabil G. Seidah   Annals of the New York Academy of Sciences

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

Clinical aspects of PCSK9

(2011) Bertrand Cariou et al.   ATHEROSCLEROSIS

Identification of proprotein convertase substrates using genome-wide expression correlation analysis

(2011) Hannu Turpeinen et al.   BMC GENOMICS

The Metabolic Serine Hydrolases and Their Functions in Mammalian Physiology and Disease

(2011) Jonathan Z. Long et al.   CHEMICAL REVIEWS

Proteolytic activation of the epithelial sodium channel and therapeutic application of a serine protease inhibitor for the treatment of salt-sensitive hypertension

(2011) Kenichiro Kitamura et al.   Clinical and Experimental Nephrology

Rosuvastatin, Proprotein Convertase Subtilisin/Kexin Type 9 Concentrations, and LDL Cholesterol Response: the JUPITER Trial

(2011) Z. Awan et al.   CLINICAL CHEMISTRY

Novel Loss-of-Function PCSK9 Variant Is Associated with Low Plasma LDL Cholesterol in a French-Canadian Family and with Impaired Processing and Secretion in Cell Culture

(2011) J. Mayne et al.   CLINICAL CHEMISTRY

Heterozygous Mutations Causing Partial Prohormone Convertase 1 Deficiency Contribute to Human Obesity

(2011) J. W. M. Creemers et al.   DIABETES

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

(2011) Paola Lo Surdo et al.   EMBO REPORTS

PCSK9: an emerging target for treatment of hypercholesterolemia

(2011) Christopher J Duff et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

The microenvironment patterns the pluripotent mouse epiblast through paracrine Furin and Pace4 proteolytic activities

(2011) D. Mesnard et al.   GENES & DEVELOPMENT

Site-1 Protease Is Essential to Growth Plate Maintenance and Is a Critical Regulator of Chondrocyte Hypertrophic Differentiation in Postnatal Mice

(2011) Debabrata Patra et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Proprotein Convertase PC7 Enhances the Activation of the EGF Receptor Pathway through Processing of the EGF Precursor

(2011) Estelle Rousselet et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Latent Transforming Growth Factor β-Binding Proteins-2 and -3 Inhibit the Proprotein Convertase 5/6A

(2011) Xiaowei Sun et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Furin Is the Major Processing Enzyme of the Cardiac-specific Growth Factor Bone Morphogenetic Protein 10

(2011) Delia Susan-Resiga et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Inactivation of endothelial proprotein convertase 5/6 decreases collagen deposition in the cardiovascular system: role of fibroblast autophagy

(2011) Chiara Marchesi et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Adamts5 (aggrecanase-2) is widely expressed in the mouse musculoskeletal system and is induced in specific regions of knee joint explants by inflammatory cytokines

(2011) James D. Wylie et al.   JOURNAL OF ORTHOPAEDIC RESEARCH

Effects of currently prescribed LDL-C-lowering drugs on PCSK9 and implications for the next generation of LDL-C-lowering agents

(2011) Robert J Konrad et al.   Lipids in Health and Disease

Phase I Trial of “bi-shRNAifurin/GMCSF DNA/Autologous Tumor Cell” Vaccine (FANG) in Advanced Cancer

(2011) Neil Senzer et al.   MOLECULAR THERAPY

PCSK9 LNA Antisense Oligonucleotides Induce Sustained Reduction of LDL Cholesterol in Nonhuman Primates

(2011) Marie W Lindholm et al.   MOLECULAR THERAPY

Genetic variants in novel pathways influence blood pressure and cardiovascular disease risk

(2011) Georg B. Ehret et al.   NATURE

Proprotein Convertases in Health and Disease

(2011) Andrew W. Artenstein et al.   NEW ENGLAND JOURNAL OF MEDICINE

Computational Reverse-Engineering of a Spider-Venom Derived Peptide Active Against Plasmodium falciparum SUB1

(2011) Giacomo Bastianelli et al.   PLoS One

A Key Enzyme in the Biogenesis of Lysosomes Is a Protease That Regulates Cholesterol Metabolism

(2011) K. Marschner et al.   SCIENCE

Cellular therapies supplement: the role of granulocyte macrophage colony-stimulating factor and dendritic cells in regulatory T-cell homeostasis and expansion

(2011) Tao Zou et al.   TRANSFUSION

Evaluation of the anti-arenaviral activity of the subtilisin kexin isozyme-1/site-1 protease inhibitor PF-429242

(2011) Antonella Pasquato et al.   VIROLOGY

Transport and equilibrium uptake of a peptide inhibitor of PACE4 into articular cartilage is dominated by electrostatic interactions

(2010) Sangwon Byun et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Increased Secretion of Lipoproteins in Transgenic Mice Expressing Human D374Y PCSK9 Under Physiological Genetic Control

(2010) Bronwen Herbert et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Associations between genetic variations in the FURIN gene and hypertension

(2010) Nanfang Li et al.   BMC Medical Genetics

The Influence of PCSK9 Polymorphisms on Serum Low-Density Lipoprotein Cholesterol and Risk of Atherosclerosis

(2010) Jean Davignon et al.   Current Atherosclerosis Reports

Proprotein Convertase Inhibitory Activities of Flavonoids Isolated from Oroxylum Indicum

(2010) S. Majumdar et al.   CURRENT MEDICINAL CHEMISTRY

Novel association to the proprotein convertase PCSK7 gene locus revealed by analysing soluble transferrin receptor (sTfR) levels

(2010) Konrad Oexle et al.   HUMAN MOLECULAR GENETICS

PCSK6 is associated with handedness in individuals with dyslexia

(2010) Thomas S. Scerri et al.   HUMAN MOLECULAR GENETICS

Inhibition of Proprotein Convertase SKI-1 Blocks Transcription of Key Extracellular Matrix Genes Regulating Osteoblastic Mineralization

(2010) Jeff P. Gorski et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

The Proprotein Convertase PC7

(2010) Estelle Rousselet et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Angiopoietin-like Protein 3 Inhibits Lipoprotein Lipase Activity through Enhancing Its Cleavage by Proprotein Convertases

(2010) Jun Liu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Imaging proprotein convertase activities and their regulation in the implanting mouse blastocyst

(2010) Daniel Mesnard et al.   JOURNAL OF CELL BIOLOGY

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

Antiviral Activity of a Small-Molecule Inhibitor of Arenavirus Glycoprotein Processing by the Cellular Site 1 Protease

(2010) S. Urata et al.   JOURNAL OF VIROLOGY

Disrupted recycling of the low density lipoprotein receptor by PCSK9 is not mediated by residues of the cytoplasmic domain

(2010) Thea Bismo Strøm et al.   MOLECULAR GENETICS AND METABOLISM

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

Subtilases: The superfamily of subtilisin-like serine proteases

(2010) Roland J. Siezen et al.   PROTEIN SCIENCE

Commentary PCSK9 variants: A new database

(2009) Sarah E.A. Leigh et al.   ATHEROSCLEROSIS

In Vivo Bioluminescence Imaging of Furin Activity in Breast Cancer Cells Using Bioluminogenic Substrates

(2009) Anca Dragulescu-Andrasi et al.   BIOCONJUGATE CHEMISTRY

Comprehensive Whole-Genome and Candidate Gene Analysis for Response to Statin Therapy in the Treating to New Targets (TNT) Cohort

(2009) John F. Thompson et al.   Circulation-Cardiovascular Genetics

Genetic Variation at the Proprotein Convertase Subtilisin/Kexin Type 5 Gene Modulates High-Density Lipoprotein Cholesterol Levels

(2009) Iulia Iatan et al.   Circulation-Cardiovascular Genetics

Running the gauntlet: an overview of the modalities of travel employed by the putative morphogen Nodal

(2009) Daniel B Constam   CURRENT OPINION IN GENETICS & DEVELOPMENT

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

(2009) Majambu Mbikay et al.   FEBS LETTERS

The role of furin in papillomavirus infection

(2009) Patricia M Day et al.   Future Microbiology

PCSK9 impedes hepatitis C virus infectionin vitroand modulates liver CD81 expression

(2009) Patrick Labonté et al.   HEPATOLOGY

Mutations and polymorphisms in the proprotein convertase subtilisin kexin 9 (PCSK9) gene in cholesterol metabolism and disease

(2009) Marianne Abifadel et al.   HUMAN MUTATION

Inhibition of Furin/Proprotein Convertase-catalyzed Surface and Intracellular Processing by Small Molecules

(2009) Tomoko Komiyama et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2009) Markey C. McNutt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Genetic and Metabolic Determinants of Plasma PCSK9 Levels

(2009) Susan G. Lakoski et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

A new method for measurement of total plasma PCSK9: clinical applications

(2009) Geneviève Dubuc et al.   JOURNAL OF LIPID RESEARCH

Potent Inhibitors of Furin and Furin-like Proprotein Convertases Containing Decarboxylated P1 Arginine Mimetics

(2009) Gero L. Becker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Neuropeptidomic analysis establishes a major role for prohormone convertase-2 in neuropeptide biosynthesis

(2009) Xin Zhang et al.   JOURNAL OF NEUROCHEMISTRY

The proprotein convertase PC5/6 is protective against intestinal tumorigenesis: in vivo mouse model

(2009) Xiaowei Sun et al.   Molecular Cancer

A chimeric LDL receptor containing the cytoplasmic domain of the transferrin receptor is degraded by PCSK9

(2009) Øystein L. Holla et al.   MOLECULAR GENETICS AND METABOLISM

MEROPS: the peptidase database

(2009) Neil D. Rawlings et al.   NUCLEIC ACIDS RESEARCH

Obesity-related Polymorphisms and Their Associations With the Ability to Regulate Fat Oxidation in Obese Europeans: The NUGENOB Study

(2009) Eva Corpeleijn et al.   Obesity

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

Different Mechanisms of Recognition and ER Retention by Transmembrane Transcription Factors CREB-H and ATF6

(2009) Marta Llarena et al.   TRAFFIC

Proprotein convertase activation of aggrecanases in cartilage in situ

(2008) Anne-Marie Malfait et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Cripto recruits Furin and PACE4 and controls Nodal trafficking during proteolytic maturation

(2008) Marie-Hélène Blanchet et al.   EMBO JOURNAL

Proprotein convertases as therapeutic targets

(2008) Michel Chrétien et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

PCSK9 as a therapeutic target of dyslipidemia

(2008) Nabil G Seidah   EXPERT OPINION ON THERAPEUTIC TARGETS

Knock-out mouse models of proprotein convertases: unique functions or redundancy?

(2008) John et al.   Frontiers in Bioscience-Landmark

VACTERL/caudal regression/Currarino syndrome-like malformations in mice with mutation in the proprotein convertase Pcsk5

(2008) D. Szumska et al.   GENES & DEVELOPMENT

Regulation of prohepcidin processing and activity by the subtilisin-like proprotein convertases Furin, PC5, PACE4 and PC7

(2008) N Scamuffa et al.   GUT

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

Proprotein convertase subtilisin/kexin type 4 in mammalian fertility: a review

(2008) Charles Gyamera-Acheampong et al.   HUMAN REPRODUCTION UPDATE

The activation and physiological functions of the proprotein convertases

(2008) N SEIDAH et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Inhibition of Chikungunya Virus Infection in Cultured Human Muscle Cells by Furin Inhibitors

(2008) Simona Ozden et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selective inhibition of proprotein convertases represses the metastatic potential of human colorectal tumor cells

(2008) Nathalie Scamuffa et al.   JOURNAL OF CLINICAL INVESTIGATION

PCSK9: a convertase that coordinates LDL catabolism

(2008) Jay D. Horton et al.   JOURNAL OF LIPID RESEARCH

Pharmacologic Inhibition of Site 1 Protease Activity Inhibits Sterol Regulatory Element-Binding Protein Processing and Reduces Lipogenic Enzyme Gene Expression and Lipid Synthesis in Cultured Cells and Experimental Animals

(2008) J. L. Hawkins et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Synthetic Small-Molecule Prohormone Convertase 2 Inhibitors

(2008) D. Kowalska et al.   MOLECULAR PHARMACOLOGY

T-cell-expressed proprotein convertase furin is essential for maintenance of peripheral immune tolerance

(2008) Marko Pesu et al.   NATURE

Common nonsynonymous variants in PCSK1 confer risk of obesity

(2008) Michael Benzinou et al.   NATURE GENETICS

Differential regulation of prohormone convertase 1/3, prohormone convertase 2 and phosphorylated cyclic-AMP-response element binding protein by short-term and long-term morphine treatment: Implications for understanding the “switch” to opiate addiction

(2008) V. Paez Espinosa et al.   NEUROSCIENCE

Molecular basis for LDL receptor recognition by PCSK9

(2008) H. J. Kwon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

In vivo functions of the proprotein convertase PC5/6 during mouse development: Gdf11 is a likely substrate

(2008) R. Essalmani et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Role of furin in granular acidification in the endocrine pancreas: Identification of the V-ATPase subunit Ac45 as a candidate substrate

(2008) E. Louagie 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

Cell-surface processing of extracellular human immunodeficiency virus type 1 Vpr by proprotein convertases

(2007) Yong Xiao et al.   VIROLOGY