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PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome.
Kroeze, Wesley K; Sassano, Maria F; Huang, Xi-Ping; Lansu, Katherine; McCorvy, John D; Giguère, Patrick M; Sciaky, Noah; Roth, Bryan L.
Affiliation
  • Kroeze WK; 1] Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA. [2] National Institute of Mental Health Psychoactive Drug Screening Program, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA.
  • Sassano MF; 1] Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA. [2] National Institute of Mental Health Psychoactive Drug Screening Program, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA.
  • Huang XP; 1] Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA. [2] National Institute of Mental Health Psychoactive Drug Screening Program, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA.
  • Lansu K; Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA.
  • McCorvy JD; Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA.
  • Giguère PM; Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA.
  • Sciaky N; Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA.
  • Roth BL; 1] Department of Pharmacology, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA. [2] National Institute of Mental Health Psychoactive Drug Screening Program, University of North Carolina, Chapel Hill, Chapel Hill, North Carolina, USA. [3] Program in Neuroscience, Universit
Nat Struct Mol Biol ; 22(5): 362-9, 2015 May.
Article in En | MEDLINE | ID: mdl-25895059
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 ß-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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Biological Assay / Receptors, G-Protein-Coupled Limits: Humans Language: En Journal: Nat Struct Mol Biol Journal subject: BIOLOGIA MOLECULAR Year: 2015 Document type: Article Affiliation country: United States Country of publication: United States
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Biological Assay / Receptors, G-Protein-Coupled Limits: Humans Language: En Journal: Nat Struct Mol Biol Journal subject: BIOLOGIA MOLECULAR Year: 2015 Document type: Article Affiliation country: United States Country of publication: United States