[4-21]Discovery of Beta-arrestin- and G Protein-biased Agonists of Dopamine D2 Receptors

报告题目:Discovery of Beta-arrestin- and G Protein-biased Agonists of Dopamine D2 Receptors

人:Jian Jin Professor, Icahn School of Medicine at Mount Sinai
报告时间:2017421日(星期)上午9:30
报告地点:独墅湖校区二期云轩楼2301

 

 

报告摘要:
G protein-coupled receptors (GPCRs) signal not only via canonical pathways involving heterotrimeric large G proteins, but also via non-canonical G protein-independent interactions with other signaling proteins includingeta-arrestins.Signaling bias (also known as functional selectivity) refers to the process by which GPCR ligands differentially modulate canonical and non-canonical signal transduction pathways. Biased agonistsof GPCRs are extremely useful for elucidating the key signal transduction pathways essential for both the therapeutic actions and side-effectsof drugs.Discoveryof eta-arrestin- and G protein-biased agonists of dopamine D2 receptors (D2R)and in vitro and in vivo characterization of these biased D2R agonists will be presented.