From methylene bridged diindole to carbonyl linked benzimidazoleindole: Development of potent and metabolically stable PCSK9 modulators

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C). Through phenotypic screening, we previously discovered a class of small-molecules with a 2,3′-diindolymethane (DIM) skeleton that can decrease th...

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Veröffentlicht in:	European journal of medicinal chemistry 2020-11, Vol.206, p.112678-112678, Article 112678
Hauptverfasser:	Xie, Haibo, Yang, Ka, Winston-McPherson, Gabrielle N., Stapleton, Donnie S., Keller, Mark P., Attie, Alan D., Smith, Kerry A., Tang, Weiping
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzimidazoles - chemistry Benzimidazoles - metabolism Benzimidazoles - pharmacokinetics Benzimidazoles - pharmacology Drug Stability Fluorine scan Humans Indole Indoles - chemistry Liver - metabolism Metabolic stability Mice PCSK9 Phenotypic screening Proprotein Convertase 9 - metabolism Rats Structure-Activity Relationship
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