Proprotein Convertase Subtilisin/Kexin 9 Inhibitors

Having excess levels of PCSK9 is not sufficient to induce complex formation between PCSK9 and the LDL receptor

(2014) Catherine J. Wooten et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Effects of Evolocumab (AMG 145), a Monoclonal Antibody to PCSK9, in Hypercholesterolemic, Statin-Treated Japanese Patients at High Cardiovascular Risk

(2014) Atsushi Hirayama et al.   CIRCULATION JOURNAL

Design and Rationale of the GAUSS-2 Study Trial: A Double-Blind, Ezetimibe-Controlled Phase 3 Study of the Efficacy and Tolerability of Evolocumab (AMG 145) in Subjects With Hypercholesterolemia Who Are Intolerant of Statin Therapy

(2014) Leslie Cho et al.   CLINICAL CARDIOLOGY

Rationale and Design of LAPLACE-2: A Phase 3, Randomized, Double-Blind, Placebo- and Ezetimibe-Controlled Trial Evaluating the Efficacy and Safety of Evolocumab in Subjects With Hypercholesterolemia on Background Statin Therapy

(2014) Jennifer G. Robinson et al.   CLINICAL CARDIOLOGY

Efficacy and safety of evolocumab (AMG 145), a fully human monoclonal antibody to PCSK9, in hyperlipidaemic patients on various background lipid therapies: pooled analysis of 1359 patients in four phase 2 trials

(2014) E. A. Stein et al.   EUROPEAN HEART JOURNAL

Lipid, blood pressure and kidney update 2013

(2014) Maciej Banach et al.   INTERNATIONAL UROLOGY AND NEPHROLOGY

Management of familial hypercholesterolemia in children and adolescents. Position paper of the Polish Lipid Expert Forum

(2014) Małgorzata Myśliwiec et al.   Journal of Clinical Lipidology

A 52-Week Placebo-Controlled Trial of Evolocumab in Hyperlipidemia

(2014) Dirk J. Blom et al.   NEW ENGLAND JOURNAL OF MEDICINE

State of the art paper Treatment of non-ST-elevation myocardial infarction and ST-elevation myocardial infarction in patients with chronic kidney disease

(2013) Beata Franczyk-Skóra et al.   Archives of Medical Science

The safety of therapeutic monoclonal antibodies: Implications for cardiovascular disease and targeting the PCSK9 pathway

(2013) A.L. Catapano et al.   ATHEROSCLEROSIS

Effect of the Proprotein Convertase Subtilisin/Kexin 9 Monoclonal Antibody, AMG 145, in Homozygous Familial Hypercholesterolemia

(2013) Evan A. Stein et al.   CIRCULATION

Efficacy and Safety of Longer-Term Administration of Evolocumab (AMG 145) in Patients With Hypercholesterolemia

(2013) Michael J. Koren et al.   CIRCULATION

PCSK9 Inhibition - A Novel Mechanism to Treat Lipid Disorders?

(2013) Maciej Banach et al.   CURRENT PHARMACEUTICAL DESIGN

Combined Dyslipidemia: Should the Focus be LDL Cholesterol or Atherogenic Dyslipidemia?

(2013) Manfredi Rizzo et al.   CURRENT PHARMACEUTICAL DESIGN

Familial hypercholesterolaemia is underdiagnosed and undertreated in the general population: guidance for clinicians to prevent coronary heart disease: Consensus Statement of the European Atherosclerosis Society

(2013) B. G. Nordestgaard et al.   EUROPEAN HEART JOURNAL

The Multifaceted Proprotein Convertases: Their Unique, Redundant, Complementary, and Opposite Functions

(2013) Nabil G. Seidah et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Management of familial heterozygous hypercholesterolemia: Position Paper of the Polish Lipid Expert Forum

(2013) Andrzej Rynkiewicz et al.   Journal of Clinical Lipidology

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

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

AMG 145, a Monoclonal Antibody Against PCSK9, Facilitates Achievement of National Cholesterol Education Program–Adult Treatment Panel III Low-Density Lipoprotein Cholesterol Goals Among High-Risk Patients

(2013) Nihar R. Desai et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Effect of an RNA interference drug on the synthesis of proprotein convertase subtilisin/kexin type 9 (PCSK9) and the concentration of serum LDL cholesterol in healthy volunteers: a randomised, single-blind, placebo-controlled, phase 1 trial

(2013) Kevin Fitzgerald et al.   LANCET

1-Year results from OSLER trial of anti-PCSK9 monoclonal antibody evolocumab

(2013) Bryony M. Mearns   Nature Reviews Cardiology

PCSK9 Prosegment Chimera as Novel Inhibitors of LDLR Degradation

(2013) Yascara Grisel Luna Saavedra et al.   PLoS One

An attempt to make lipid-lowering therapy more effective in Hungary. The results of MULTI GAP 2010 and the Plus Program

(2012) Laszlo Mark et al.   Archives of Medical Science

State of the art papers Lipids, blood pressure, kidney – what was new in 2011?

(2012) Marcin Barylski et al.   Archives of Medical Science

Editorial Lipid-lowering therapies and achievement of LDL-cholesterol targets

(2012) Manfredi Rizzo et al.   Archives of Medical Science

Low-Density Lipoprotein Cholesterol–Lowering Effects of AMG 145, a Monoclonal Antibody to Proprotein Convertase Subtilisin/Kexin Type 9 Serine Protease in Patients With Heterozygous Familial Hypercholesterolemia

(2012) Frederick Raal et al.   CIRCULATION

Antibodies to PCSK9

(2012) Kara N. Maxwell et al.   CIRCULATION RESEARCH

Inhibition of pre-protein convertase serine kexin-9 (PCSK-9) as a treatment for hyperlipidaemia

(2012) Anthony S Wierzbicki et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

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

Effect of a Monoclonal Antibody to PCSK9 on Low-Density Lipoprotein Cholesterol Levels in Statin-Intolerant Patients

(2012) David Sullivan et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Increasing Serum Half-life and Extending Cholesterol Loweringin Vivoby Engineering Antibody with pH-sensitive Binding to PCSK9

(2012) Javier Chaparro-Riggers et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The PCSK9 decade

(2012) Gilles Lambert et al.   JOURNAL OF LIPID RESEARCH

Effects of AMG 145 on Low-Density Lipoprotein Cholesterol Levels

(2012) Clapton S. Dias et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

RETRACTED: Plasma PCSK9 Levels and Clinical Outcomes in the TNT (Treating to New Targets) Trial

(2012) Roeland Huijgen et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 as monotherapy in patients with hypercholesterolaemia (MENDEL): a randomised, double-blind, placebo-controlled, phase 2 study

(2012) Michael J Koren et al.   LANCET

Effect of a Monoclonal Antibody to PCSK9 on LDL Cholesterol

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

The Role of Proprotein Convertase Subtilisin/Kexin Type 9 in Hyperlipidemia

(2011) Michel Farnier   American Journal of Cardiovascular Drugs

Editorial Are we getting to lipid targets in real life?

(2011) Niki Katsiki et al.   Archives of Medical Science

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

Proprotein convertase subtilisin kexin type 9 (PCSK9) secreted by cultured smooth muscle cells reduces macrophages LDLR levels

(2011) Nicola Ferri et al.   ATHEROSCLEROSIS

Future issues, public policy, and public awareness of Familial Hypercholesterolemias: Recommendations from the National Lipid Association Expert Panel on Familial Hypercholesterolemia

(2011) Anne C. Goldberg et al.   Journal of Clinical Lipidology

Familial Hypercholesterolemia: Screening, diagnosis and management of pediatric and adult patients

(2011) Anne C. Goldberg et al.   Journal of Clinical Lipidology

Effects of statin treatment on endothelial function, oxidative stress and inflammation in patients with arterial hypertension and normal cholesterol levels

(2011) Niki Katsiki et al.   JOURNAL OF HYPERTENSION

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

(2011) Marie W Lindholm et al.   MOLECULAR THERAPY

Pharmacological strategies for lowering LDL cholesterol: statins and beyond

(2011) Ariel Brautbar et al.   Nature Reviews Cardiology

Current prospects for RNA interference-based therapies

(2011) Beverly L. Davidson et al.   NATURE REVIEWS GENETICS

Proprotein convertase subtilisin/kexin type 9 (PCSK9): From structure–function relation to therapeutic inhibition

(2011) G. Tibolla et al.   NUTRITION METABOLISM AND CARDIOVASCULAR DISEASES

Beyond LDL Cholesterol, a New Role for PCSK9

(2010) Omar N. Akram et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

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

(2010) Jean Davignon et al.   Current Atherosclerosis Reports

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

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

High-dose atorvastatin causes a rapid sustained increase in human serum PCSK9 and disrupts its correlation with LDL cholesterol

(2010) Greg Welder et al.   JOURNAL OF LIPID RESEARCH

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

Adnectins: engineered target-binding protein therapeutics

(2010) D. Lipovsek   PROTEIN ENGINEERING DESIGN & SELECTION

Evaluation of cholesterol lowering treatment of patients with familial hypercholesterolemia: a large cross-sectional study in The Netherlands

(2009) A.H. Pijlman et al.   ATHEROSCLEROSIS

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

(2009) Christopher J. Duff et al.   BIOCHEMICAL JOURNAL

Longitudinal Association of PCSK9 Sequence Variations With Low-Density Lipoprotein Cholesterol Levels

(2009) Chiang-Ching Huang et al.   Circulation-Cardiovascular Genetics

Plasma PCSK9 Is Associated with Age, Sex, and Multiple Metabolic Markers in a Population-Based Sample of Children and Adolescents

(2009) A. Baass et al.   CLINICAL CHEMISTRY

EUROASPIRE III: a survey on the lifestyle, risk factors and use of cardioprotective drug therapies in coronary patients from 22 European countries

(2009) Kornelia Kotseva et al.   EUROPEAN JOURNAL OF CARDIOVASCULAR PREVENTION & REHABILITATION

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

(2009) Majambu Mbikay et al.   FEBS LETTERS

Hepatocyte Nuclear Factor 1α Plays a Critical Role inPCSK9Gene Transcription and Regulation by the Natural Hypocholesterolemic Compound Berberine

(2009) Hai Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2009) S. A. Mousavi et al.   JOURNAL OF INTERNAL MEDICINE

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

(2009) Geneviève Dubuc 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

Inhibition of PCSK9: A powerful weapon for achieving ideal LDL cholesterol levels

(2009) D. Steinberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular basis of PCSK9 function

(2008) Gilles Lambert et al.   ATHEROSCLEROSIS

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

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

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