October 2022 "Psychedelics, also known as classical hallucinogens, affect processes related to perception, cognition and sensory processing mostly via the serotonin 5-HT2A receptor (5-HT2AR). This class of psychoactive substances, which includes lysergic acid diethylamide (LSD), psilocybin, mescaline and the substituted amphetamine 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), is receiving renewed attention for their potential therapeutic properties as it relates to psychiatric conditions such as depression and substance use disorders. Current studies focused on the potentially clinical effects of psychedelics on human subjects tend to exclude sex as a biological variable. Much of the understanding of psychedelic pharmacology is derived from rodent models, but most of this preclinical research has only focused on male mice. Here we tested the effects of DOI on head-twitch behavior (HTR) - a mouse behavioral proxy of human psychedelic potential - in male and female mice. DOI elicited more HTR in female as compared to male C57BL/6J mice, a sex-specific exacerbated behavior that was not observed in 129S6/SvEv animals. Volinanserin (or M100907) - a 5-HT2AR antagonist - fully prevented DOI-induced HTR in male and female C57BL/6J mice. Accumulation of inositol monophosphate (IP1) in the frontal cortex upon DOI administration showed no sex-related effect in C57BL/6J mice. However, the pharmacokinetic properties of DOI differed among sexes - brain and plasma concentrations of DOI were lower 30 and 60 min after drug administration in female as compared to male C57BL/6J mice. Together, these results suggest strain-dependent and sex-related differences in the behavioral and pharmacokinetic profiles of the 5-HT2AR agonist DOI in C57BL/6J mice, and support the importance of studying sex as a biological variable in preclinical psychedelic research." Read more at the source #DrGPCR #GPCR #IndustryNews

intracellular domain dictate and condition long-term GPCR activities associated with the regulation of protein understanding of this function of GPCRs is likely to significantly augment our ability to further employ these proteins

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. As activation and recruitment of effector proteins might influence each other, thorough analysis of bias Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements

Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but Not G Protein Interaction "The calcium-sensing receptor is a homodimeric class C G protein-coupled receptor (GPCR) senses extracellular Ca2+ (Ca2+o ) via a dimeric extracellular Venus flytrap (VFT) unit that activates G protein-dependent

August 2022 "The calcium-permeable cation channel TRPM3 can be activated by heat and the endogenous steroid pregnenolone sulfate. TRPM3's best understood function is its role as a peripheral noxious heat sensor in mice. However, the channel is expressed in various tissues and cell types including neurons as well as glial and epithelial cells. TRPM3 expression patterns differ between species and change during development. Furthermore, a plethora of TRPM3 variants that result from alternative splicing have been identified and the majority of these isoforms are yet to be characterized. Moreover, the mechanisms underlying regulation of TRPM3 are largely unexplored. In addition, a micro-RNA gene (miR-204) is located within the TRPM3 gene. This complexity makes it difficult to obtain a clear picture of TRPM3 characteristics. However, a clear picture is needed to unravel TRPM3's full potential as experimental tool, diagnostic marker and therapeutic target. Therefore, the newest data related to TRPM3 have to be discussed and to be put in context as soon as possible to be up-to-date and to accelerate the translation from bench to bedside. The aim of this review is to highlight recent results and developments with particular focus on findings from studies involving ocular tissues and cells or peripheral neurons of rodents and humans." Read more at the source #DrGPCR #GPCR #IndustryNews

, transient multiprotein assemblies, and individual molecules of complex proteins. substates of conformationally complex proteins. Potential for protein crystallization: Nanobodies can be used to stabilize the protomers of larger protein This provides a better starting point for the crystallization of intrinsically unfolded proteins. Nanobodies to Study G Protein-Coupled Receptor Structure and Function.

"Protecting neurons from death during oxidative and neuroexcitotoxic stress is key for preventing cognitive involving interaction between neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled cells with NF-α1/CPE increased pERK 1/2 and pCREB levels which prevented a decrease in pro-survival protein Cell survival assay in β-arrestin Knockout HEK293 cells showed that the NF-α1/CPE-5-HTR1E-mediated protection Importantly, knock-down of 5-HTR1E in human primary neurons diminished the NF-α1/CPE-mediated protection

András Tóth , László Hunyady , et al. for their work on G protein-coupled receptor endocytosis generates the   Classified GPCR News  from June 24th to 30th, 2024 Adhesion GPCRs Novel Isoforms of Adhesion G Protein-Coupled Characterized by an Integrative Biophysical Approach Redox-modulated SNX25 as a novel regulator of GPCR-G protein cingulate cortex modulates decision making in rats Translation-independent association of mRNAs encoding protomers and Molecular Insights into GPCR Function Structural basis for hormone recognition and distinctive Gq protein

Matthew T Eddy and his team's research on A2A adenosine receptor activation by G protein and mutations GPCR Activation and Signaling DANGER Signals Activate G -Protein Receptor Kinases Suppressing Neutrophil After Tissue Trauma Single-molecule visualization of human A2A adenosine receptor activation by a G protein structure prediction using a protein language model Reviews, GPCRs, and more Potential of olfactory complex Deep Learning Dynamic Allostery of G-Protein-Coupled Receptors Industry News Sosei Heptares

Adhesion GPCRs The adhesion G-protein-coupled receptor mayo/CG11318 controls midgut development in Drosophila A method for structure determination of GPCRs in various states Reviews, GPCRs, and more G Protein-coupled Showcase™ 2024 Establishing our first international translational research project - Institute for Protein Novartis Salipro Biotech announces multi-target research collaboration with an additional Top5 crop protection Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein

Adhesion GPCRs Dual role of the adhesion G-protein coupled receptor ADRGE5/CD97 in glioblastoma invasion Functions and mechanisms of the GPCR adaptor protein Norbin. G protein-coupled receptor-mediated membrane targeting of PLCγ2 is essential for neutrophil chemotaxis GPCRs in Oncology and Immunology Interplay between G protein-coupled receptors and nanotechnology. GPCR Research Strategies for acquisition of resonance assignment spectra of highly dynamic membrane proteins

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

macrophages, including the ragulator complex (involved in nutrient stress sensing), glycosylation enzymes, protein The highest scoring protective hits included the complement C3a receptor (C3aR), a G-protein coupled

forming a vicious cycle with IGF1/IGF1R signaling pathway "There is a potential correlation between G-protein-coupled receptor-associated sorting protein 1 (GASP1) and breast tumorigenesis. Mechanistically, GASP1 inhibited proteasomal degradation of insulin-like growth factor 1 receptor (IGF1R

GPCR Activation and Signaling Single transmembrane GPCR modulating proteins: neither single nor simple platform Salipro Biotech Expands Global Intellectual Property Portfolio with Granted Patent in Japan Proteros (June 28 - 30, 2023) NEW FREE Seminar Antibodies targeting Membrane Proteins - From Antigen to New Therapeutics November 2 - 4, 2023) Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels, and Transport Proteins

Adhesion GPCRs Functional partnerships between GPI-anchored proteins and adhesion GPCRs GPCR Activation dynamic simulations Kinetic insights into agonist-dependent signalling bias at the pro-inflammatory G-protein Current and emerging methods for probing neuropeptide transmission Nanowire Biosensors with Olfactory Proteins Pharmaceuticals Closes $115 Million Loan Facility with Hercules Capital Gene-to-structure and Europe give Proteros November 20 -23, 2023) Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels, and Transport Proteins

crucial for understanding the diverse signaling outcomes mediated by different receptors including G protein In the endosomes, sustained G protein signaling has been associated with prolonged interactions between GPCRs, G proteins, and arrestins on endosomal membranes3,4. Additionally, the conditions within endosomes, such as low pH and high protease activity, can degrade Nuclear G-protein-coupled receptors as putative novel pharmacological targets.

G protein-coupled receptors (GPCRs) are a vast family of membrane-bound proteins crucial for transmitting avoiding interactions with non-cognate G proteins [1]. Gq proteins could bolster Gs dependent-β2-adrenergic receptor-mediated cAMP signalling, while Gs proteins prepare the GPCR in a manner that optimizes subsequent cognate G protein activation. landscape where non-cognate G proteins play a critical preparatory role.

October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by

Remodeling in the Remote Myocardium of Rats After an Acute Myocardial Infarction by Activating β-Arrestin-2, Protein Their remote myocardia showed increased mRNA and protein levels of collagen I/III with higher levels They also showed higher protein levels of phospho-glycogen synthase kinase-3β (p-GSK3β), as well as total levels of Bcl-2, β-arrestin-2, and protein phosphatase-2 (PP2A). Interestingly, Exendin-4 increased mRNA levels of MnSOD, protein levels of β-arrestin-2 and PP2A, and

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 Concurrently, the α1 helix extends, propagating structural changes throughout the G protein. Physiological roles of G protein-coupled receptor kinases and arrestins. Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).

G protein-coupled receptors (GPCRs) are integral membrane proteins crucial for sensing extracellular Resonance Energy Transfer (BRET), has revolutionized the study of GPCRs by enabling real-time monitoring of protein-protein Wan, Q., et al., Mini G protein probes for active G protein-coupled receptors (GPCRs) in live cells.  Eidne, Bioluminescence resonance energy transfer (BRET) for the real-time detection of protein-protein Nat Protoc, 2006. 1(1): p. 337-45. 15.   

One fascinating aspect of the cellular signaling network is the crosstalk between G protein-coupled receptors involvement in a myriad of physiological processes, mediate mostly signaling through heterotrimeric G proteins The researchers focused on the phosphorylation of the G protein subunit Gαi at specific residues within The ability of growth factors to modulate G protein signaling through specific phosphorylation events For instance, the sequestration of G proteins from canonical GPCR-dependent pathways by growth factor

CXV: The Class F of G Protein-Coupled Receptors Yusman Manchanda , Dr. Alejandra Tomas , et al. for their research on Engineered mini-G proteins block the internalization of receptor drug discovery The application of targeted protein degradation technologies to G protein-coupled receptors Unravelling G protein-coupled receptor signalling networks using global phosphoproteomics CXV: The Class F of G Protein-Coupled Receptors Structural and Molecular Insights into GPCR Function

GPCR Activation and Signaling Tail engagement of arrestin at the glucagon receptor Gα protein signaling Taste Gβγ-SNAP25 exocytotic brake removal enhances insulin action, promotes adipocyte browning, and protects November 20 -23, 2023) Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels, and Transport Proteins

Garcia-Marcos for their work on Get ready to sharpen your tools:A short guide to heterotrimeric G protein Michel Bouvier , et al. for their study on the Role of the V2R-βarrestin-Gβγ complex in promoting G protein independent desensitization mechanisms Get ready to sharpen your tools:A short guide to heterotrimeric G protein chagas disease vector Rhodnius Prolixus (Stål ) Role of the V2R-βarrestin-Gβγ complex in promoting G protein Receptor Influence of the Water Model on the Structure and Interactions of the GPR40 Protein with the

ligands via nanobody tethering Elk Kossatz, Michel Bouvier, Jana Selent, et al. for their study on G protein-specific Signaling Highly biased agonism for GPCR ligands via nanobody tethering Mechanistic insights into G-protein Webinars June 2 - 7, 2024 | Chemotactic Cytokines June 4, 2024 | Live Webinar ‘It All Starts With a Protein – Protein Sciences as a Key to Success in Drug Discovery’ June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics

Oncology and Immunology Molecular docking and dynamics simulation studies uncover the host-pathogen protein-protein interactions in Penaeus vannamei and Vibrio parahaemolyticus Involvement of Protease-Activated Receptor2 Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein