Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor

被引：22
|
作者：
Bohn, Laura M. [1 ,2 ]
Aube, Jeffrey [3 ]
机构：
[1] Scripps Res Inst, Dept Mol Med, Jupiter, FL 33458 USA
[2] Scripps Res Inst, Dept Neurosci, Jupiter, FL 33458 USA
[3] Univ North Carolina Chapel Hill, UNC Eshelman Sch Pharm, Div Chem Biol & Med Chem, Chapel Hill, NC 27599 USA
来源：
ACS MEDICINAL CHEMISTRY LETTERS | 2017年 / 8卷 / 07期
关键词：
beta Arrestin; biased ligands; functional selectivity; G protein-coupled receptors; kappa opioid receptor agonists; PROTEIN-COUPLED RECEPTORS; STRUCTURE-BASED DISCOVERY; GPCR DRUG DISCOVERY; 6'-GUANIDINONALTRINDOLE 6'-GNTI; FUNCTIONAL SELECTIVITY; NOR-BINALTORPHIMINE; KINASE-C; AGONIST; ANTAGONIST; ASTROCYTES;
D O I：
10.1021/acsmedchemlett.7b00224
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The discovery and characterization of two classes of kappa opioid receptor agonists that are biased for G protein over beta arrestin signaling are described.
引用
收藏
页码：694 / 700
页数：7
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