PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome. Nat Struct Mol Biol 2015 May;22(5):362-9
Date
04/22/2015Pubmed ID
25895059Pubmed Central ID
PMC4424118DOI
10.1038/nsmb.3014Scopus ID
2-s2.0-84929285245 (requires institutional sign-in at Scopus site) 604 CitationsAbstract
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 β-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.
Author List
Kroeze WK, Sassano MF, Huang XP, Lansu K, McCorvy JD, Giguère PM, Sciaky N, Roth BLAuthor
John McCorvy PhD Associate Professor in the Cell Biology Neurobiology and Anatomy department at Medical College of WisconsinMESH terms used to index this publication - Major topics in bold
Amino Acid SequenceArrestins
Biological Assay
Humans
Ligands
RNA Interference
RNA, Small Interfering
Receptors, G-Protein-Coupled
Transcription, Genetic
Transcriptional Activation
beta-Arrestins
