Matches in SemOpenAlex for { <https://semopenalex.org/work/W4383264311> ?p ?o ?g. }
- W4383264311 abstract "Representing the most attractive and successful druggable receptors of the proteome, GPCRs regulate a myriad of physiological and pathophysiological functions. Although over half of present pharmaceuticals target GPCRs, the advancement of drug discovery is hampered by a lack of adequate screening tools, the majority of which are limited to probing agonist-induced G-protein and β-arrestin-2-mediated events as a measure of receptor activation. Here, we develop Tango-Trio, a comprehensive cell-based high-throughput platform comprising cumate-inducible expression of transducers, capable of the parallelized profiling of both basal and agonist-dependent GPCR activities. We capture the functional diversity of GPCRs, reporting β-arrestin-1/2 couplings, selectivities, and receptor internalization signatures across the GPCRome. Moreover, we present the construction of cumate-induced basal activation curves at approximately 200 receptors, including over 50 orphans. Overall, Tango-Trio's robustness is well-suited for the functional characterization and screening of GPCRs, especially for parallel interrogation, and is a valuable addition to the pharmacological toolbox." @default.
- W4383264311 created "2023-07-06" @default.
- W4383264311 creator A5027851192 @default.
- W4383264311 creator A5037235711 @default.
- W4383264311 creator A5040964231 @default.
- W4383264311 creator A5074354899 @default.
- W4383264311 creator A5080015317 @default.
- W4383264311 date "2023-07-05" @default.
- W4383264311 modified "2023-10-14" @default.
- W4383264311 title "Profiling of basal and ligand-dependent GPCR activities by means of a polyvalent cell-based high-throughput platform" @default.
- W4383264311 cites W1531611091 @default.
- W4383264311 cites W1603274157 @default.
- W4383264311 cites W1607594420 @default.
- W4383264311 cites W1718009280 @default.
- W4383264311 cites W1872581706 @default.
- W4383264311 cites W1942734748 @default.
- W4383264311 cites W1967509058 @default.
- W4383264311 cites W1988097700 @default.
- W4383264311 cites W2002137514 @default.
- W4383264311 cites W2007791463 @default.
- W4383264311 cites W2021929569 @default.
- W4383264311 cites W2027144764 @default.
- W4383264311 cites W2036251618 @default.
- W4383264311 cites W2039229115 @default.
- W4383264311 cites W2043297755 @default.
- W4383264311 cites W2049648432 @default.
- W4383264311 cites W2055417411 @default.
- W4383264311 cites W2074239574 @default.
- W4383264311 cites W2076261565 @default.
- W4383264311 cites W2079523532 @default.
- W4383264311 cites W2081929369 @default.
- W4383264311 cites W2083808584 @default.
- W4383264311 cites W2085879736 @default.
- W4383264311 cites W2088175248 @default.
- W4383264311 cites W2094843483 @default.
- W4383264311 cites W2096756239 @default.
- W4383264311 cites W2102849876 @default.
- W4383264311 cites W2107282910 @default.
- W4383264311 cites W2110386073 @default.
- W4383264311 cites W2116265895 @default.
- W4383264311 cites W2142456569 @default.
- W4383264311 cites W2149298399 @default.
- W4383264311 cites W2151526347 @default.
- W4383264311 cites W2154927219 @default.
- W4383264311 cites W2157562973 @default.
- W4383264311 cites W2158187739 @default.
- W4383264311 cites W2160898059 @default.
- W4383264311 cites W2162337394 @default.
- W4383264311 cites W2163371429 @default.
- W4383264311 cites W2170494228 @default.
- W4383264311 cites W2186153196 @default.
- W4383264311 cites W2222077151 @default.
- W4383264311 cites W2233644193 @default.
- W4383264311 cites W2256040435 @default.
- W4383264311 cites W2300047490 @default.
- W4383264311 cites W2354094227 @default.
- W4383264311 cites W2589991249 @default.
- W4383264311 cites W2593419978 @default.
- W4383264311 cites W2626714978 @default.
- W4383264311 cites W2734817732 @default.
- W4383264311 cites W2768273109 @default.
- W4383264311 cites W2801577207 @default.
- W4383264311 cites W2802239966 @default.
- W4383264311 cites W2885422782 @default.
- W4383264311 cites W2886980930 @default.
- W4383264311 cites W2889163572 @default.
- W4383264311 cites W2899198283 @default.
- W4383264311 cites W2914089449 @default.
- W4383264311 cites W2944810644 @default.
- W4383264311 cites W2965912723 @default.
- W4383264311 cites W2996405687 @default.
- W4383264311 cites W3010864411 @default.
- W4383264311 cites W3037707998 @default.
- W4383264311 cites W3100178082 @default.
- W4383264311 cites W3121684188 @default.
- W4383264311 cites W3130063272 @default.
- W4383264311 cites W3146761575 @default.
- W4383264311 cites W3156551585 @default.
- W4383264311 cites W3199710005 @default.
- W4383264311 cites W3209896479 @default.
- W4383264311 cites W4220763721 @default.
- W4383264311 cites W4245103782 @default.
- W4383264311 cites W88161901 @default.
- W4383264311 doi "https://doi.org/10.1038/s41467-023-39132-x" @default.
- W4383264311 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/37407564" @default.
- W4383264311 hasPublicationYear "2023" @default.
- W4383264311 type Work @default.
- W4383264311 citedByCount "1" @default.
- W4383264311 countsByYear W43832643112023 @default.
- W4383264311 crossrefType "journal-article" @default.
- W4383264311 hasAuthorship W4383264311A5027851192 @default.
- W4383264311 hasAuthorship W4383264311A5037235711 @default.
- W4383264311 hasAuthorship W4383264311A5040964231 @default.
- W4383264311 hasAuthorship W4383264311A5074354899 @default.
- W4383264311 hasAuthorship W4383264311A5080015317 @default.
- W4383264311 hasBestOaLocation W43832643111 @default.
- W4383264311 hasConcept C104317684 @default.
- W4383264311 hasConcept C10679952 @default.
- W4383264311 hasConcept C135285700 @default.
- W4383264311 hasConcept C139770010 @default.