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• W3204847843 endingPage "10638" @default.
• W3204847843 startingPage "10638" @default.
• W3204847843 abstract "G-protein-coupled receptors (GPCRs) are dimeric proteins, but the functional consequences of the process are still debated. Active GPCR conformations are promoted either by agonists or constitutive activity. Inverse agonists decrease constitutive activity by promoting inactive conformations. The histamine H3 receptor (H3R) is the target of choice for the study of GPCRs because it displays high constitutive activity. Here, we study the dimerization of recombinant and brain H3R and explore the effects of H3R ligands of different intrinsic efficacy on dimerization. Co-immunoprecipitations and Western blots showed that H3R dimers co-exist with monomers in transfected HEK 293 cells and in rodent brains. Bioluminescence energy transfer (BRET) analysis confirmed the existence of spontaneous H3R dimers, not only in living HEK 293 cells but also in transfected cortical neurons. In both cells, agonists and constitutive activity of the H3R decreased BRET signals, whereas inverse agonists and GTPγS, which promote inactive conformations, increased BRET signals. These findings show the existence of spontaneous H3R dimers not only in heterologous systems but also in native tissues, which are able to adopt a number of allosteric conformations, from more inactive to more active states." @default.
• W3204847843 created "2021-10-11" @default.
• W3204847843 creator A5019881287 @default.
• W3204847843 creator A5048695064 @default.
• W3204847843 creator A5053509756 @default.
• W3204847843 creator A5075690711 @default.
• W3204847843 date "2021-09-30" @default.
• W3204847843 modified "2023-10-03" @default.
• W3204847843 title "BRET Analysis of GPCR Dimers in Neurons and Non-Neuronal Cells: Evidence for Inactive, Agonist, and Constitutive Conformations" @default.
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• W3204847843 doi "https://doi.org/10.3390/ijms221910638" @default.
• W3204847843 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8508734" @default.
• W3204847843 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34638980" @default.
• W3204847843 hasPublicationYear "2021" @default.
• W3204847843 type Work @default.
• W3204847843 sameAs 3204847843 @default.

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