August 2022 RAB-Symposium - Regulatory Autoantibodies Targeting GPCRs. September 15-16, 2022. gives me great pleasure to announce the fourth hybrid symposium on regulatory autoantibodies targeting G-protein-coupled receptors (GPCRs) in Lübeck. GPCRs are involved in a variety of physiological and pathophysiological processes. Read more at the source #DrGPCR #GPCR #IndustryNews

The purpose of this study was to evaluate the role of dual transactivation of EGF and TGF-β receptors In addition, as an intermediary of G protein-coupled receptor (GPCR) signaling, the functions of ROCK Proteins were investigated<br />by western blotting using protein-specific antibodies against phospho-Smad2 Moreover, ET-1-increased protein expression of PAI-1 was decreased in the presence of bosentan (ET receptor Read more at the source #DrGPCR #GPCR #IndustryNews

G protein-coupled receptors (GPCRs) are integral membrane proteins crucial for sensing extracellular Gilman, A.G., G proteins: transducers of receptor-generated signals.  Wan, Q., et al., Mini G protein probes for active G protein-coupled receptors (GPCRs) in live cells.  McNeill, S.M., et al., The role of G protein-coupled receptor kinases in GLP-1R β-arrestin recruitment Namkung, Y., et al., Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using

Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases "The chemokine receptor CXCR3 is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies, in particular autoimmune diseases. Read more at the source #DrGPCR #GPCR #IndustryNews

2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR the gut-brain axis, have entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR) targets with a goal of creating new drug discovery programs in the area of gastrointestinal diseases. " Read more at the source #DrGPCR #GPCR #IndustryNews

protein-coupled receptors Dr. GPCR Activation and Signaling Emerging modes of regulation of neuromodulatory G protein-coupled receptors course at hippocampal CA1 synapses Regulator of G protein signaling 6 (RGS6) in dopamine neurons promotes therapeutics in targeting G protein-coupled receptors: Recent advances and challenges Structural and Events, Meetings, and Webinars June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling

4,5-bisphosphate (PI(4,5)P2) lipids have been shown to stabilize an active conformation of class A G-protein coupled receptors (GPCRs) through a conserved binding site, not present in class B GPCRs. with the Glucagon receptor (GCGR), which constitutes an important target for diabetes and obesity therapeutics conformation of GCGR through a binding site conserved across class B GPCRs but absent in class A GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

One fascinating aspect of the cellular signaling network is the crosstalk between G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs). The cross-talk between growth factor receptors and GPCRs is an intriguing area of study. C Terminus (Tyr320): Phosphorylation at Tyr320 disrupted Gβγ binding, receptor coupling, and ligand-stimulated Growth factor-dependent phosphorylation of Gαi shapes canonical signaling by G protein-coupled receptors

signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR smoothened "The oncogenic G-protein-coupled receptor (GPCR) Smoothened (SMO) is a key transducer of This effect involves the sequential and additive action of protein kinase A, casein kinase I, and the of HH to the apico-basal distribution of SMO and provide a novel mechanism for the regulation of a GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

G protein-coupled receptors (GPCRs) are a vast family of membrane-bound proteins crucial for transmitting Using BRET based approaches, the Gs-coupled vasopressin V2 receptor (V2R) was shown to form a stable This unproductive coupling revealed that non-cognate G protein interactions could modulate GPCR signalling coupling efficiency of cognate G proteins to GPCRs, thereby amplifying canonical downstream signalling , facilitating subsequent coupling of cognate G proteins and promoting enhanced signalling.

Bell-Evans model and steered molecular dynamics in uncovering the dissociation kinetics of ligands targeting G-protein-coupled receptors "Recently, academic and industrial scientific communities involved in kinetics-based drug absolute residence times of the antagonist ZMA241385 and agonist NECA that target the A2A adenosine receptor of the G-protein-coupled receptor (GPCR) protein family. Read more at the source #DrGPCR #GPCR #IndustryNews

Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel biosensor shed light on the endosomal proteome associated with the δ-opioid receptor (DOR). This study, published in Nature Chemical Biology, highlights the role of the chaperone protein DNAJC13 In this study, the DOR receptor was genetically fused to APEX2, creating a DOR-APEX2 construct. the endosomal proteome associated with the DOR receptor.

Before the advent of AlphaFold, homology modeling was the most common method for predicting G protein-coupled receptor (GPCR) structures, especially when experimental data were limited. the target protein ( Carlsson, J. et al., 2011 ). , a notable challenge for GPCRs. To fully understand GPCR behavior and optimize drug targeting across multiple receptor states, experimental

We previously demonstrated that the G protein-coupled receptor (GPCR) arginine vasopressin receptor type1A AVPR1A is part of a family of GPCR's including arginine vasopressin receptor type 2 (AVPR2). Stimulation of AVPR2 with a selective agonist desmopressin promoted CRPC cell proliferation through cAMP/protein kinase A signaling, consistent with AVPR2 coupling to the G protein subunit alpha s. Read more at the source #DrGPCR #GPCR #IndustryNews

2022 "Numerous physiological processes in insects are tightly regulated by neuropeptides and their receptors form an ancient signaling system, there is still a great deal of variety in neuropeptides and their receptors Neuropeptides and their receptors have been documented in many hemipteran insects, but the differences Here, 33 neuropeptide precursors and 48 putative neuropeptide G protein-coupled receptor (GPCR) genes Read more at the source #DrGPCR #GPCR #IndustryNews

This assay was applied to various target classes, with particular emphasis on those for which protein-based In one example, to study a G protein coupled receptor (GPCR), we used one antagonist as probe and multiple Read more at the source #DrGPCR #GPCR #IndustryNews

Class B G protein-coupled receptors (GPCRs) are notoriously difficult to target by small molecules because Using the parathyroid hormone type 1 receptor (PTHR) as a prototypic class B GPCR target, and a combination Here we found a key mechanical site that modulates the collective dynamics of the receptor and used this precise druggable sites and identify allosteric modulators of PTHR signaling that could be extended to GPCRs

Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone Peptide-Derived G Protein Coupled Receptor Agonists "The increasing prevalence of obesity and type 2 diabetes (T2DM) is protein-coupled receptors (GPCR). Great success has been reached with therapies based on the GLP-1 receptor monoagonism; therefore, a logical Read more at the source #DrGPCR #GPCR #IndustryNews

Human cells express over 800 G-protein-coupled receptors (GPCRs) to facilitate communication with the Capturing the dynamics of GPCR activation has always been a challenge because G protein activation in protein from the receptor. Physiological roles of G protein-coupled receptor kinases and arrestins. Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).

2022 Ono Enters into Collaboration Agreement with Domain Therapeutics and Université de Montréal for GPCR-Targeted Domain”) and Université de Montréal (Québec, Canada; “UdM”), to discover novel small molecules targeting G-Protein Coupled Receptors (GPCRs) in a metabolic disease area." Read more at the source #DrGPCR #GPCR #IndustryNews

G protein-coupled receptors (GPCRs) transduce a diverse variety of extracellular stimuli into intracellular The β2-adrenergic receptor (β2AR) is a prototypical and extensively studied GPCR that can provide insight SIGNIFICANCE STATEMENT: The role of extracellular G protein-coupled receptor (GPCR) domains in mediating with G protein and β-arrestin. with G protein and β-arrestin with a biased loss of β-arrestin binding.

August 2022 "Chemokines, a subgroup of cytokines along with their receptors, are involved in various C-X-C motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "While the role of G-protein-coupled receptors (GPCR) in cancer is acknowledged, their underlying Protease-activated receptors (PAR), a subgroup of GPCRs, form a family of four members (PAR1-4) centrally In addition to PH-Akt/PKB association, other PH-containing signal proteins such as Gab1 and Sos1 also AYPGKF peptide ligand activation of PAR4 induces EGF receptor (EGFR) Tyr-phosphorylation, effectively Read more at the source #DrGPCR #GPCR #IndustryNews

Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors APJ receptors form both homodimers and heterodimers with other members of the class A GPCR family such PAFR as a model, showing that stabilization of PAFR oligomers promotes G protein activity, and decreases G proteins and therefore preserve their physiological functions, an important observation when considering GPCR drugs efficacy usually depends on a pathway (G protein or β-arrestin), whereas side effects are

G protein-coupled receptors (GPCRs) are critical myocardial signal transducers which regulate cardiac therapeutics currently used in HF target these receptors. A recent focus on GPCR intracellular-regulating proteins such as GPCR kinases (GRKs) has uncovered GRK2 Additionally, the GRK2 interactome includes numerous proteins which interact with differential domains Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "GPCR signaling and function depend on their associated proteins and subcellular locations Besides G-proteins and β-arrestins, 14-3-3 proteins participate in GPCR trafficking and signaling, and they connect a large number of diverse proteins to form signaling networks. could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal a new approach for GPCR drug development by modulating GPCR/14-3-3 signals temporally."

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially Although GPCRs are primarily found at the plasma membrane, GPCRs can traffic to and signal from many CXC chemokine receptor 3 (CXCR3). Endosomal signaling is critical for biased activation of G proteins, β-arrestins, and extracellular-signal-regulated and other GPCRs."

Odorant receptors function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR) family and are the largest known mammalian gene family with around 900 genes. OR51E1 and OR51E2, initially assumed to be GPCRs only expressed in prostate tissue, play a role in prostate compounds, there has been a growing interest from the scientific community to target this class of GPCRs Check the original article at https://pubmed.ncbi.nlm.nih.gov/35999088/ #GPCR #DrGPCR#Ecosystem