Literature DB >> 25782778

The promise of proprotein convertase subtilisin/kexin 9 inhibitors for the treatment of familial hypercholesterolemia.

Yashashwi Pokharel1, Salim S Virani, Christie M Ballantyne.   

Abstract

Familial hypercholesterolemia comprises a constellation of genetic disorders resulting in very high cholesterol levels since childhood. If untreated, it is associated with accelerated atherosclerosis and premature cardiovascular disease. It has been shown that if aggressive cholesterol lowering is achieved in familial hypercholesterolemia, the incidence of cardiovascular disease can be lowered. However, currently approved pharmacological therapies are not able to lower cholesterol to optimal levels in a large number of these patients. Proprotein convertase subtilisin/kexin 9 inhibitors are a new class of cholesterol-lowering medications that can significantly reduce cholesterol levels in these patients especially those with at least some functioning low-density lipoprotein receptors. In this article, we will briefly review familial hypercholesterolemia and the role of proprotein convertase subtilisin/kexin 9 inhibitors in this condition.

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Year:  2015        PMID: 25782778     DOI: 10.1007/s11883-015-0508-7

Source DB:  PubMed          Journal:  Curr Atheroscler Rep        ISSN: 1523-3804            Impact factor:   5.113


  46 in total

Review 1.  Lipid lowering with PCSK9 inhibitors.

Authors:  Razvan T Dadu; Christie M Ballantyne
Journal:  Nat Rev Cardiol       Date:  2014-06-24       Impact factor: 32.419

2.  Safety and efficacy of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 serine protease, SAR236553/REGN727, in patients with primary hypercholesterolemia receiving ongoing stable atorvastatin therapy.

Authors:  James M McKenney; Michael J Koren; Dean J Kereiakes; Corinne Hanotin; Anne-Catherine Ferrand; Evan A Stein
Journal:  J Am Coll Cardiol       Date:  2012-03-28       Impact factor: 24.094

3.  Effect of a monoclonal antibody to PCSK9, REGN727/SAR236553, to reduce low-density lipoprotein cholesterol in patients with heterozygous familial hypercholesterolaemia on stable statin dose with or without ezetimibe therapy: a phase 2 randomised controlled trial.

Authors:  Evan A Stein; Dan Gipe; Jean Bergeron; Daniel Gaudet; Robert Weiss; Robert Dufour; Richard Wu; Robert Pordy
Journal:  Lancet       Date:  2012-05-26       Impact factor: 79.321

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

Authors:  Kara N Maxwell; Edward A Fisher; Jan L Breslow
Journal:  Proc Natl Acad Sci U S A       Date:  2005-01-27       Impact factor: 11.205

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

Authors:  Thomas A Lagace; David E Curtis; Rita Garuti; Markey C McNutt; Sahng Wook Park; Heidi B Prather; Norma N Anderson; Y K Ho; Robert E Hammer; Jay D Horton
Journal:  J Clin Invest       Date:  2006-11       Impact factor: 14.808

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

Authors:  Sahng Wook Park; Young-Ah Moon; Jay D Horton
Journal:  J Biol Chem       Date:  2004-09-22       Impact factor: 5.157

Review 7.  Safety and effect of very low levels of low-density lipoprotein cholesterol on cardiovascular events.

Authors:  John C LaRosa; Terje R Pedersen; Ransi Somaratne; Scott M Wasserman
Journal:  Am J Cardiol       Date:  2013-01-30       Impact factor: 2.778

8.  Genome-wide expression analysis of cells expressing gain of function mutant D374Y-PCSK9.

Authors:  Trine Ranheim; Morten Mattingsdal; Jessica M Lindvall; Oystein L Holla; Knut Erik Berge; Mari Ann Kulseth; Trond P Leren
Journal:  J Cell Physiol       Date:  2008-11       Impact factor: 6.384

9.  The effects of single- and multiple-dose administration of bococizumab (RN316/PF-04950615), a humanized IgG2Δa monoclonal antibody binding proprotein convertase subtilisin/kexin type 9, in hypercholesterolemic subjects treated with and without atorvastatin: Results from four phase I studies.

Authors:  Barry Gumbiner; Tenshang Joh; Hong Liang; Hong Wan; Matteo Levisetti; Alicia M Vana; David L Shelton; Philippe Forgues; Stephan Billotte; Jaume Pons; Charles M Baum; Pamela D Garzone
Journal:  Cardiovasc Ther       Date:  2017-11-23       Impact factor: 3.023

10.  Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor.

Authors:  Yingnan Zhang; Charles Eigenbrot; Lijuan Zhou; Steven Shia; Wei Li; Clifford Quan; Jeffrey Tom; Paul Moran; Paola Di Lello; Nicholas J Skelton; Monica Kong-Beltran; Andrew Peterson; Daniel Kirchhofer
Journal:  J Biol Chem       Date:  2013-11-13       Impact factor: 5.157

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