FRET and BRET sensors operate on the principle of energy transfer between a fluorescent or luminescent One of the significant advantages of FRET and BRET-based sensors is their ability to provide real-time BERKY consists of a membrane linker, a BRET donor, an ER/K α-helix linker, a BRET acceptor, and an active Lee, Probing Arrestin Function Using Intramolecular FlAsH-BRET Biosensors.  Goyet, E., et al., Fast and high resolution single-cell BRET imaging. 

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization, internalization, and signaling. The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated functions. Here, we provide evidence that distal carboxyl-terminal tail (C-tail), but not proximal, phosphorylation of the chemokine receptor CXCR4 specifies βarrestin1 (βarr1)-dependent signaling. We demonstrate by pharmacologic inhibition of GRK2/3-mediated phosphorylation of the chemokine receptor CXCR4 coupled with site-directed mutagenesis and bioluminescence resonance energy transfer approaches that distal, not proximal, C-tail phosphorylation sites are required for recruitment of the adaptor protein STAM1 (signal-transducing adaptor molecule) to βarr1 and focal adhesion kinase phosphorylation but not extracellular signal-regulated kinase 1/2 phosphorylation. In addition, we show that GPCRs that have similarly positioned C-tail phosphoresidues are also able to recruit STAM1 to βarr1. However, although necessary for some GPCRs, we found that distal C-tail sites might not be sufficient to specify recruitment of STAM1 to βarr1 for other GPCRs. In conclusion, this study provides evidence that distal C-tail phosphorylation sites specify GRK-βarrestin-mediated signaling by CXCR4 and other GPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous peptide GPR15L(25-81) and a C-terminal peptide fragment GPR15L(71-81). GPR15 signals through the Gi/o pathway to decrease intracellular cyclic adenosine 3',5'-monophosphate (cAMP). However, the activation profiles of the GPR15 receptor within Gi/o subtypes have not been examined. Moreover, whether the receptor can also couple to Gs , Gq/11 and G12/13 is unclear. Here, GPR15L(25-81) and GPR15L(71-81) are used as pharmacological tool compounds to delineate the GPR15 receptor-mediated Gα protein signalling using a G protein activation assay and second messenger assay conducted on living cells. The results show that the GPR15 receptor preferentially couples to Gi/o rather than other pathways in both assays. Within the Gi/o family, the GPR15 receptor activates all the subtypes (Gi1 , Gi2 , Gi3 , GoA , GoB and Gz ). The Emax and activation rates of Gi1, Gi2 , Gi3, GoA and GoB are similar, whilst the Emax of Gz is smaller and the activation rate is significantly slower. The potencies of both peptides toward each Gi/o subtype have been determined. Furthermore, the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked by the application of the Gi/o inhibitor pertussis toxin." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Enzymatic and cellular signalling biosensors are used to decipher the activities of complex biological systems. Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in the human body, are plentiful and vary in utility, form and function. Their applications have continually expanded our understanding of this important protein class. Here, we briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling and selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric signalling complexes." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE

31,32] The 1992 Nobel Prize in Physiology or Medicine was awarded to Edwin Gerhard Krebs and Edmond Henri Histamine pharmacology: from Sir Henry Dale to the 21st century.

be used for a range of different applications, including bioluminescence resonance energy transfer (BRET

., for their work on Conformation- and activation-based BRET sensors differentially report on GPCR-G Cell-Surface and Endomembrane-Exclusive β-Adrenergic Receptor Signaling Conformation- and activation-based BRET

Gunnar Schulte , for their study on Class-Wide Analysis of Frizzled-Dishevelled Interactions Using BRET modulation by allosteric antagonists Class-Wide Analysis of Frizzled-Dishevelled Interactions Using BRET

Regarding GRKs role in CCR2 scavenging, BRET, flow cytometry and fluorescence microscopy readouts revealed The ability to rapidly recycle, which was shown by a chemokine washout BRET assay (Y.

employed a series of phospho-mimicking mutants and assays such as linear ion trap mass spectrometry, BRET

Using BRET based approaches, the Gs-coupled vasopressin V2 receptor (V2R) was shown to form a stable

Research using techniques like bioluminescence resonance energy transfer (BRET) and fluorescence resonance

Methods & Updates in GPCR Research NanoBiT- and NanoBiT/BRET-based assays allow the analysis of binding

congrats to: John Teye Azietaku for his first contributor article on Illuminating GPCR Research: FRET and BRET-Based

Moreover, Förster resonance energy transfer (FRET), bioluminescence resonance energy transfer (BRET),