Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the

We confirmed that this phenomenon of rapidly decreasing agonist-induced GPCR/14-3-3 signal intensity

NanoBRETTM studies to determine protein–protein interaction were conducted, confirming decreased homodimerization

Of these, four fragment- and seven lead-like compounds were confirmed to bind to the allosteric site

Of these, four fragment- and seven lead-like compounds were confirmed to bind to the allosteric site

Furthermore, univariate analysis confirmed that GPER was a significant prognostic factor for DMFS in

These interactions induce local conformational changes which are amplified and transmitted to the intracellular the structure-activity data obtained for the ensemble of candidate hits provides a rich resource of information to inform lead optimization, either by human and in silico-aided rational design, or by the construction For more information, follow Orion Biotechnology on LinkedIn or visit www.orionbiotechnology.com.

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We show that epitope-tagged GCGRs undergo clathrin- and dynamin-dependent endocytosis in HEK293 and Huh