via enhancing NLRP3 inflammasome activation in macrophages "The putative medium-chain free fatty acid receptor GPR84 is a G protein-coupled receptor primarily expressed in myeloid cells that constitute the innate Consistently, GPR84-/- mice are resistant to the development of colitis induced by DSS. These results define a unique role of GPR84 in innate immune cells and intestinal inflammation, and suggest Read more at the source #DrGPCR #GPCR #IndustryNews

receptors, remain unknown. 1 receptor (CB1). remains unclear. Prompted by these results, we investigated the role of the CBD compound on the CB1 receptor using similar domain of the CB1 receptor.

September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer , and receptor internalization. Our results reveal that the extended N-terminus of the long isoform limits G protein activation yet elevates receptor-β-arrestin interaction. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Class A (rhodopsin-like) G protein-coupled receptors (GPCRs) are constitutive phospholipid scramblases as evinced after their reconstitution into liposomes. Yet phospholipid scrambling is not detectable in the resting plasma membrane of mammalian cells that is replete with GPCRs. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G-protein-coupled receptors (GPCRs) are involved in a wide array of physiological and disease functions, yet knowledge of their role in colon cancer stem cell maintenance is still lacking In addition, the molecular mechanisms underlying GPCR-induced post-translational signaling regulation Taken together, we reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases We hypothesized that there is a common set of receptor interactions made by ligands of diverse structures β2AR structures, generating ca 75 000 docking poses and predicted all atomic interactions between the receptor This approach can be readily applied to any drug target." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid receptor-dependent Although increasing evidence has suggested the direct role of fentanyl on cancer, little is known on Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Abstract Rodent models are commonly used to evaluate parathyroid hormone (PTH) and PTH-related Divergence, however, in the amino acid sequences of rodent and human PTH receptors (rat and mouse PTH1Rs for such ligands when assessed on rodent vs human PTH1Rs, as shown by cell-based assays in vitro. To overcome this potential uncertainty, we used a homologous recombination-based knockin (KI) approach Read more at the source #DrGPCR #GPCR #IndustryNews

Kunitz-type snake toxin family associated with an original mode of interaction with the vasopressin 2 receptor "Abstract Background and purpose: Venomous animals express numerous Kunitz-type peptides. Key results: Eight additional MQs were identified with nanomolar affinities for the V2R, all antagonists The variant MQ1-K39A showed a higher affinity for the hV2R, but not for the rat V2R. Read more at the source #DrGPCR #GPCR #IndustryNews

G protein-coupled receptors (GPCRs) have been shown to play integral roles in Alzheimer's disease pathogenesis As signaling via the GPCRs, β2-adrenergic receptor (β2AR), and metabotropic glutamate receptor 2 (mGluR2 ) promotes hyperphosphorylation of tau, we hypothesized that β-arrestin1 represents a point of convergence tauopathy and rescues impaired synaptic plasticity and cognitive impairments in PS19 mice. Read full article

receptors. Ligand recognition and activation of neuromedin U receptor 2. receptor. Receptor. July 2 - 7. Explore Dr. GPCR Ecosystem

Stay informed with the most recent developments in GPCR research and industry news. the second round. GPCR Activation and Signaling Emerging modes of regulation of neuromodulatory G protein-coupled receptors G protein-coupled receptors: Recent advances and challenges Structural and Molecular Insights into GPCR Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics US 2024 October 2

Negative allosteric modulation of the glucagon receptor by RAMP2. Itch receptor MRGPRX4 interacts with the receptor activity-modifying proteins (RAMPs). Regulator of G-Protein Signalling 4 (RGS4) negatively modulates nociceptin/orphanin FQ opioid receptor Cannabinoid Tolerance in S426A/S430A x β-Arrestin 2 Knockout Double-Mutant Mice. (July 2 - 7, 2023). 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023) GPCR Jobs NEW Convergent

Hello Readers👋, Get the latest GPCR News more frequently directly in your inbox and in the Ecosystem D5R, highly expressed in CA1 hippocampal neurons, selectively reduces CaV 3.2 and CaV 3.3 currents GPCR Receptor Reviews, GPCRs, and more Life, death and resurrection of plant GPCRs Structural and Molecular Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology. July 2 - 7. Explore Dr. GPCR Ecosystem

Rational Drug Design One immediate application of this research lies in rational drug design . create drugs that precisely modulate receptor responses. residues , which affect nearby regions but do not make active state-specific contacts. receptor function indirectly. R., ... & Manglik, A. (2024).

A conserved intracellular allosteric binding site (IABS) has recently been identified at several G protein-coupled receptors (GPCRs). Starting from vercirnon, an intracellular C-C chemokine receptor type 9 (CCR9) antagonist and previous In a proof-of-principle study, we succeeded in showing that our CCR9-PROTAC is able to reduce CCR9 levels Read full article

body temperature, cardiovascular homeostasis, reproduction, and inflammation. Recent studies have revealed that PGs play pivotal roles in embryo development, ciliogenesis, and organ Prostaglandins are also essential for skeletal muscle repair. This review outlines recent advances in understanding the functions and mechanisms of prostaglandin signaling Read full article

transcriptomics and peptidomics of central nervous system identify neuropeptides and their G protein-coupled receptors Neuropeptides and their specific receptors (primarily G protein-coupled receptors, GPCRs) regulate multiple biological functions in insects and represent promising next-generation pest management strategy. Taken together, these results will benefit further investigations to determine physiological functions Read full article

potential therapeutic benefits, including greater pharmacodynamic specificity, increased efficiency and reduced The biased signaling modulation of non-GPCR receptors has yet to be exploited. Toll-like receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent In this review, we aim to provide an overview of the recent progress in the discovery of biased modulators Read full article

December 2021 Crinetics Pharmaceuticals announced the formation of an independently operated new company, Radionetics Radionetics aims to develop a deep pipeline of novel, targeted, nonpeptide radiopharmaceuticals for the Radionetics aims to develop a deep pipeline of novel, targeted, nonpeptide radiopharmaceuticals for the treatment of a broad range of oncology indications." Read more at the source #DrGPCR #GPCR #IndustryNews

Efferocytes release extracellular vesicles to resolve inflammation and tissue injury via prosaposin-GPR37 Methods & Updates in GPCR Research Evaluation of Drug Responses to Human β2AR Using Native Mass Spectrometry Reviews, GPCRs, and more Optical approaches for investigating neuromodulation and G Protein-Coupled Receptor Hijacking of GPCRs and RTKs by pathogens. (November 2 - 4, 2023) Registration is now open!

signaling pathway in primary Sjögren's syndrome The etiology of primary Sjögren's syndrome (pSS) remains β-arrestin2 is a key protein that mediates desensitization and internalization of G protein-coupled receptors (GPCRs) and it participates in inflammatory and immune responses that have been found to mediate apoptosis This research further clarified the underlying role of β-arrestin2 and provided an experimental foundation Read full article

Remember, the early-bird registration and Abstract submission deadline is September 8, and the final ability to respond to progesterone: a study based on RNA-seq Reviews, GPCRs, and more Tri-part NanoLuc (November 2 - 4, 2023) MPGPCR Conference (November 15 -17, 2023) ASCEPT Annual Scientific Meeting (November Laboratory Specialist Associate NEW Postdoc Research Associate Director, Regulatory Affairs Research Robert Lefkowitz Lab Postdoc Fellow - Dr. Robert Lefkowitz Lab Explore Dr. GPCR Ecosystem

Bryan Roth, Sudarshan Rajagopal, and Graeme Milligan. Save the date! Dr. The relaxin receptor RXFP1 signals through a mechanism of autoinhibition. Regulation of the pro-inflammatory G protein-coupled receptor GPR84. GPCR Binders, Drugs, and more Development of a 5-HT7 receptor antibody for the rat: the good, the bad (July 2 - 7, 2023). 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023) GPCR Jobs NEW Postdoctoral

Stay informed with the most recent developments in GPCR research and industry news. and regulation Dr. Submit your logo and review the rules. The contest deadline is August 15th, 2024. in living cells Reviews, GPCRs, and more Restoring function to inactivating G protein-coupled receptor Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics US 2024 October 2

Let's explore the newest developments in GPCR research and community news together! reserve your spot in our upcoming course ! reveal a discrete cellular mechanism of endosomal G protein activation Amylin receptor subunit interactions of G protein-coupled receptors GPCRs in Cardiology, Endocrinology, and Taste Latrophilin-2 Deletion conformational changes in the β1-adrenergic receptor revealed by hydrogen-deuterium exchange mass spectrometry

Get ready to save the dates! Dr. Revealing the graded activation mechanism of neurotensin receptor 1 Intracellular pathways of calcitonin gene-related peptide-induced relaxation of human coronary arteries: A key role for Gβγ subunit instead The receptor tyrosine kinase IGF1R and its associated GPCRs are co-regulated by the noncoding RNA NEAT1 - The value of GPCR cell-based assays in drug discovery October 2024 | Biologics US 2024   October 2

The role of intracellular calcium and Rho kinase pathways in G protein-coupled receptor-mediated contractions Ligand for β3-Adrenergic Receptor. Reviews, GPCRs, and more Pharmacological Profiling of a Brugia malayi Muscarinic Acetylcholine Receptor (July 2 - 7, 2023). Assistant Research Fellow - School of Physics and Astronomy Postdoctoral Research Associate (Fixed Term