PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome

G protein-coupled receptors (GPCRs) are essential mediators of cellular signaling and important targets of drug action. Of the approximately 350 non-olfactory human GPCRs, more than 100 are still considered “orphans” as their endogenous ligand(s) remain unknown. Here, we describe a unique open-sourc...

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Autores principales: Kroeze, W.K., Sassano, M.F., Huang, X.-P., Lansu, K., McCorvy, J.D., Giguere, P.M., Sciaky, N., Roth, B.L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4424118/
https://www.ncbi.nlm.nih.gov/pubmed/25895059
http://dx.doi.org/10.1038/nsmb.3014
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author Kroeze, W.K.
Sassano, M.F.
Huang, X.-P.
Lansu, K.
McCorvy, J.D.
Giguere, P.M.
Sciaky, N.
Roth, B.L.
author_facet Kroeze, W.K.
Sassano, M.F.
Huang, X.-P.
Lansu, K.
McCorvy, J.D.
Giguere, P.M.
Sciaky, N.
Roth, B.L.
author_sort Kroeze, W.K.
collection PubMed
description G protein-coupled receptors (GPCRs) are essential mediators of cellular signaling and important targets of drug action. Of the approximately 350 non-olfactory human GPCRs, more than 100 are still considered “orphans” as their endogenous ligand(s) remain unknown. Here, we describe a unique open-source resource that provides the capacity to interrogate the druggable human GPCR-ome via a G protein-independent β-arrestin recruitment assay. We validate this unique platform at more than 120 non-orphan human GPCR targets, demonstrate its utility for discovering new ligands for orphan human GPCRs, and describe a method (PRESTO-TANGO; Parallel Receptor-ome Expression and Screening via Transcriptional Output - TANGO) for the simultaneous and parallel interrogation of the entire human GPCR-ome.
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spelling pubmed-44241182015-11-01 PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome Kroeze, W.K. Sassano, M.F. Huang, X.-P. Lansu, K. McCorvy, J.D. Giguere, P.M. Sciaky, N. Roth, B.L. Nat Struct Mol Biol Article G protein-coupled receptors (GPCRs) are essential mediators of cellular signaling and important targets of drug action. Of the approximately 350 non-olfactory human GPCRs, more than 100 are still considered “orphans” as their endogenous ligand(s) remain unknown. Here, we describe a unique open-source resource that provides the capacity to interrogate the druggable human GPCR-ome via a G protein-independent β-arrestin recruitment assay. We validate this unique platform at more than 120 non-orphan human GPCR targets, demonstrate its utility for discovering new ligands for orphan human GPCRs, and describe a method (PRESTO-TANGO; Parallel Receptor-ome Expression and Screening via Transcriptional Output - TANGO) for the simultaneous and parallel interrogation of the entire human GPCR-ome. 2015-04-20 2015-05 /pmc/articles/PMC4424118/ /pubmed/25895059 http://dx.doi.org/10.1038/nsmb.3014 Text en http://www.nature.com/authors/editorial_policies/license.html#terms Users may view, print, copy, and download text and data-mine the content in such documents, for the purposes of academic research, subject always to the full Conditions of use:http://www.nature.com/authors/editorial_policies/license.html#terms
spellingShingle Article
Kroeze, W.K.
Sassano, M.F.
Huang, X.-P.
Lansu, K.
McCorvy, J.D.
Giguere, P.M.
Sciaky, N.
Roth, B.L.
PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome
title PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome
title_full PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome
title_fullStr PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome
title_full_unstemmed PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome
title_short PRESTO-TANGO: an open-source resource for interrogation of the druggable human GPCR-ome
title_sort presto-tango: an open-source resource for interrogation of the druggable human gpcr-ome
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4424118/
https://www.ncbi.nlm.nih.gov/pubmed/25895059
http://dx.doi.org/10.1038/nsmb.3014
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