Search Results

GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. Generation of Gαi knock-out HEK293 cells illuminates Gαi-coupling diversity of GPCRs. Papers GPCRs: Signal Transduction. Deadline February 12, 2023 GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit GPCR Ecosystem

B. Nibbs et al. 2013). Volpe et al. 2012; B. N. Zhao et al. 2019). Although some GPCRs constitutively internalize through clathrin-coated pits independently of phosphorylation In this study, it is revealed that CCR2 scavenging role was largely independent of the classical GPCR Check the original article at https://pubmed.ncbi.nlm.nih.gov/36719944/ #GPCR #DrGPCR#Ecosystem

Reviews, GPCRs, and more Olfactory Receptors as an Emerging Chemical Sensing Scaffold. Christopher Prior, as CEO and Reports Recent Drug Discovery Highlights Call for GPCR Papers GPCRs: Signal GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit, (February 21 - 23, 2023) GPCR Jobs Postdoctoral Fellow - Molecular Dynamics Postdoc in lipid regulation of GPCRs Postdoctoral GPCR Ecosystem

October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered activation mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of diseases, but few therapies have been directed against GPCRs in the field of cancer, partly because of the lack Here, using colorectal cancer (CRC) as a model, we explored the gene expression of a panel of GPCRs in Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Negative Allosteric Modulator, ORG27569, and Analogs "A growing number of G-protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR podcast is here! 🎧Hear Dr. GPCR Ecosystem membership or listen wherever you get your podcast for free.

GPCRs are not suitable for antibody use due to steric hindrance and reverse binding, thus, other strategies This modification is small enough to not affect GPCR expression or activity.[21–23] The Tag-lite® binding It has been applied to different GPCR binding assays, such as CXCR4, opioid receptors, CCK1 and CCK2. R.; Martin, B. R.; Abood, M. E. Protein-Protein Interaction Analysis with Time-Resolved FRET and Snap-Tag Technologies: Application to GPCR

August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases, and arrestins - preferentially bind active GPCRs. Our analysis suggests that the structures of GPCRs bound to these interaction partners available today In view of this, three possibilities are conceivable: (i) there are no generalizable GPCR conformations Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated reveal an interaction between the βarr2 finger loop domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR podcast is now available! Our guest is Dr. Tim De Groof! It’s not often when you get the best of both worlds - nano-bodies and #GPCRs. Listen where you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast #gpcr #drgpcr #podcast

September 2022 Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5 homo- and hetero-dimer formation "The process of GPCR dimerization can have profound effects on GPCR activation, signaling, and intracellular trafficking. Somatostatin receptors (SSTs) are class A GPCRs abundantly expressed in pituitary tumors where they represent Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular Modulating a single function of a specific aGPCR isoform while affecting no other function and no other Here, we engineered an antibody, termed LK30, that binds to the extracellular region of the aGPCR ADGRL3 Our work provides proof of concept for the modulation of isoform- and ligand specific aGPCR functions therapeutics" Read more at the source #DrGPCR #GPCR #IndustryNews

However, the detailed mechanism of aGPCR activation remains elusive. The structures also unveil the rarely explored GPCR/G12 and GPCR/G13 engagements. Taken together, our study fills the missing information of GPCR/G-protein engagement and provides a framework for understanding aGPCR activation and GPR110 signaling." Read more at the source #DrGPCR #GPCR #IndustryNews

Hello GPCR Trailblazers, This week, we’re spotlighting Celtarys Research, our newest partner, featured Maria Majellaro, highlighting their fluorescent ligand tools for live-cell GPCR assays.   GPCR Updates Terry’s Corner Is Coming – Get Early Access and Updates    Terry’s Corner is launching Explore Terry's Corner From Chemistry Lab to GPCR Partner – New Podcast with Celtarys Dr. GPCR Team

Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE

GPCR Symposium on GPCR Activation and Signaling held on May 19th, 2023. Adhesion GPCRs Optimized genetic code expansion technology for time-dependent induction of adhesion GPCR-ligand GPCRs in Neuroscience Arrestin-dependent nuclear export of phosphodiesterase 4D promotes GPCR-induced Reviews, GPCRs, and more NMR applications to GPCR recognition by peptide ligands. GPCR Ecosystem

October 2022 "G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one endogenous ligands (orthosteric site), allosteric modulators offer new avenues for the regulation of GPCR Recent advances in the structure determination of GPCRs bound to different types of allosteric modulators In this review, we provide a systematic analysis of the currently available GPCR structures in complex Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR Podcast, we have Dr. Pina Cardarelli, CSO of GPCR Therapeutics. ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr#drgpcr #podcast

GPCR Summit 2022 is less than a month away! Come live and breathe GPCRs with us and don’t forget to submit your abstract. ➡️https://bit.ly/3Q7hlnT #gpcr #drgpcr

GPCR podcast! Give it a listen to hear from Dr. Thomas P. Sakmar on how the molecular studies of rhodopsin paved the way to understanding #GPCRs Be sure to subscribe https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #drgpcr #gpcr #podcast

regulating the dynamics of the serotonin1A receptor, a crucial neurotransmitter G protein-coupled receptor (GPCR in understanding the modulatory role of the membrane environment on the organization and dynamics of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

Imagine you're navigating a vast terrain—not on foot, but through the shape-shifting world of GPCRs.

By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR Virtual Cafe session with Dr. Matthew E. on Friday, October 7th at 1 PM ET.

Joe Clayton from BioTek Instruments talk about automated micro-plate-based methods for quantifying #GPCR activation. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #drgpcr #gpcr #virtualcafe

We found that some agonist-induced GPCR/14-3-3 signal intensities can rapidly decrease. could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach for GPCR drug development by modulating GPCR/14-3-3 signals temporally." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated 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. Read more at the source #DrGPCR #GPCR #IndustryNews

Introduction Cannabinoid receptors are GPCRs, and two main types exist, CB1R and CB2R. for CB1R in live cells and the PHERAstar FSX is the ideal microplate reader for characterizing the GPCR-ligand Palomares B et al. , Δ9-Tetrahydrocannabinolic acid alleviates collagen-induced arthritis: Role of PPARγ