期刊
NATURE STRUCTURAL & MOLECULAR BIOLOGY
卷 22, 期 5, 页码 362-U28出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/nsmb.3014
关键词
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资金
- US National Institutes of Health [R01DA27170, UO1MH104974]
- US National Institute of Mental Health Psychoactive Drug Screening Program
- Michael Hooker Distinguished Professorship
- University of North Carolina Department of Pharmacology Training Program [NIH 5-T32-GM007040]
G protein-coupled receptors (GPCRs) are essential mediators of cellular signaling and are important targets of drug action. Of the approximately 350 nonolfactory human GPCRs, more than 100 are still considered to be 'orphans' because their endogenous ligands remain unknown. Here, we describe a unique open-source resource that allows interrogation of the druggable human GPCRome via a G protein-independent beta-arrestin-recruitment assay. We validate this unique platform at more than 120 nonorphan human GPCR targets, demonstrate its utility for discovering new ligands for orphan human GPCRs and describe a method (parallel receptorome expression and screening via transcriptional output, with transcriptional activation following arrestin translocation (PRESTO-Tango)) for the simultaneous and parallel interrogation of the entire human nonolfactory GPCRome.
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