Identification of a PCSK9-LDLR disruptor peptide with in vivo function

Author:

Brousseau Margaret E.,Clairmont Kevin B.ORCID,Spraggon Glen,Flyer Alec N.,Golosov Andrei A.,Grosche Philipp,Amin Jakal,Andre Jerome,Burdick Debra,Caplan Shari,Chen Guanjing,Chopra Raj,Ames Lisa,Dubiel Diana,Fan Li,Gattlen Raphael,Kelly-Sullivan Dawn,Koch Alexander W.,Lewis Ian,Li Jingzhou,Liu Eugene,Lubicka Danuta,Marzinzik Andreas,Nakajima Katsumasa,Nettleton DavidORCID,Ottl Johannes,Pan Meihui,Patel Tajesh,Perry Lauren,Pickett Stephanie,Poirier Jennifer,Reid Patrick C.,Pelle Xavier,Seepersaud Mohindra,Subramanian Vanitha,Vera Victoria,Xu Mei,Yang Lihua,Yang Qing,Yu Jinghua,Zhu Guoming,Monovich Lauren G.

Funder

Novartis Institutes for BioMedical Research

Novartis

Publisher

Elsevier BV

Subject

Clinical Biochemistry,Drug Discovery,Pharmacology,Molecular Biology,Molecular Medicine,Biochemistry

Reference49 articles.

1. Anti-proprotein Convertase Subtilisin Kexin Type 9 (Anti-pcsk9) Compounds and Methods of Using the Same in the Treatment and/or Prevention of Cardiovascular Diseases;Abdel-Meguid,2017

2. Mutations in PCSK9 cause autosomal dominant hypercholesterolemia;Abifadel;Nat. Genet.,2003

3. LDL-R promoting activity of peptides derived from human PCSK9 catalytic domain (153-421): design, synthesis and biochemical evaluation;Alghamdi;Eur. J. Med. Chem.,2015

4. Series of novel and highly potent cyclic peptide PCSK9 inhibitors derived from an mRNA display screen and optimized via structure-based design;Alleyne;J. Med. Chem.,2020

5. A receptor-mediated pathway for cholesterol homeostasis;Brown;Science,1986

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