Discovery and Characterization of a G Protein–Biased Agonist That Inhibits b-Arrestin Recruitment to the D2 Dopamine Receptor
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چکیده
S Discovery and Characterization of a G Protein–Biased Agonist That Inhibits b-Arrestin Recruitment to the D2 Dopamine Receptor R. Benjamin Free, Lani S. Chun, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, Jennie L. Conroy, Adrian Padron, Julie A. Meade, Jingbo Xiao, Xin Hu, Andrés E. Dulcey, Yang Han, Lihua Duan, Steve Titus, Melanie Bryant-Genevier, Elena Barnaeva, Marc Ferrer, Jonathan A. Javitch, Thijs Beuming, Lei Shi, Noel T. Southall, Juan J. Marugan, and David R. Sibley 96
منابع مشابه
Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor.
A high-throughput screening campaign was conducted to interrogate a 380,000+ small-molecule library for novel D2 dopamine receptor modulators using a calcium mobilization assay. Active agonist compounds from the primary screen were examined for orthogonal D2 dopamine receptor signaling activities including cAMP modulation and β-arrestin recruitment. Although the majority of the subsequently con...
متن کاملMol090563 96..105
A high-throughput screening campaign was conducted to interrogate a 380,0001 small-molecule library for novel D2 dopamine receptor modulators using a calcium mobilization assay. Active agonist compounds from the primary screen were examined for orthogonal D2 dopamine receptor signaling activities including cAMPmodulation and b-arrestin recruitment. Although themajority of the subsequently confi...
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Arrestins mediate desensitization and internalization of G protein-coupled receptors and also direct receptor signaling toward heterotrimeric G protein-independent signaling pathways. We previously identified a four-residue segment (residues 212-215) of the dopamine D2 receptor that is necessary for arrestin binding in an in vitro heterologous expression system but that also impairs receptor ex...
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Agonist: a ligand that, by binding a receptor, increases that receptor’s activity. Antagonist: a ligand that binds a receptor without stimulating any activity. Also known as a ’blocker’ because of its ability to prevent binding of other ligands and, therefore, block agonist-induced activity. Correlated efficacies: when ligand binding stimulates or inhibits all receptor functions to an equal ext...
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