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 in...

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Hlavní autoři: Free, R. Benjamin, Chun, Lani S., Moritz, Amy E., Miller, Brittney N., Doyle, Trevor B., Conroy, Jennie L., Padron, Adrian, Meade, Julie A., Xiao, Jingbo, Hu, Xin, Dulcey, Andrés E., Han, Yang, Duan, Lihua, Titus, Steve, Bryant-Genevier, Melanie, Barnaeva, Elena, Ferrer, Marc, Javitch, Jonathan A., Beuming, Thijs, Shi, Lei, Southall, Noel T., Marugan, Juan J., Sibley, David R.
Médium: Artigo
Jazyk:Inglês
Vydáno: The American Society for Pharmacology and Experimental Therapeutics 2014
Témata:
Accelerated Communication
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4054005/
https://ncbi.nlm.nih.gov/pubmed/24755247
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/mol.113.090563
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