Design of Organo-Peptides As Bipartite PCSK9 Antagonists

Proprotein convertase subtilisin/kexin 9 (PCSK9) has become an important therapeutic target for lipid lowering, since it regulates low-density lipoprotein cholesterol (LDL-c) levels by binding to liver LDL receptors (LDLR) and effecting their intracellular degradation. However, the development of sm...

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Veröffentlicht in:	ACS chemical biology 2020-02, Vol.15 (2), p.425-436
Hauptverfasser:	Burdick, Daniel J, Skelton, Nicholas J, Ultsch, Mark, Beresini, Maureen H, Eigenbrot, Charles, Li, Wei, Zhang, Yingnan, Nguyen, Huy, Kong-Beltran, Monica, Quinn, John G, Kirchhofer, Daniel
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Crystallography, X-Ray Drug Design Hep G2 Cells Humans Molecular Structure Peptides - chemistry Peptides - metabolism Peptides - pharmacology Proprotein Convertase 9 - antagonists & inhibitors Proprotein Convertase 9 - chemistry Proprotein Convertase 9 - metabolism Protein Binding Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - metabolism Serine Proteinase Inhibitors - pharmacology
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