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Here we report that neuropeptide S (NPS) signaling in the PVT is necessary for stimulus salience encoding

biotech company with a unique portfolio of CB1 inverse agonists, today announces the appointment of Glenn S. Vraniak served as Chief Financial Officer of Evaxion Biotech A/S, an AI enabled immuno-oncology company

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin

Objective: The goal of this study was to determine the glucometabolic effects of acute activation of Gs signaling in skeletal muscle (SKM) in vivo and its contribution to whole-body glucose homeostasis. Methods: To address this question, we studied mice that express a Gs-coupled designer G protein-coupled receptor (Gs-DREADD or GsD) selectively in skeletal muscle. We also identified two Gs-coupled GPCRs that are endogenously expressed by SKM at relatively high levels (β2-adrenergic receptor and CRF2 receptor) and studied the acute metabolic effects of activating these receptors in vivo by highly selective agonists (clenbuterol and urocortin 2 (UCN2), respectively). Results: Acute stimulation of GsD signaling in SKM impaired glucose tolerance in lean and obese mice by decreasing glucose uptake selectively into SKM. The acute metabolic effects following agonist activation of β2-adrenergic and, potentially, CRF2 receptors appear primarily mediated by altered insulin release. Clenbuterol injection improved glucose tolerance by increasing insulin secretion in lean mice. In SKM, clenbuterol stimulated glycogen breakdown. UCN2 injection resulted in decreased glucose tolerance associated with lower plasma insulin levels. The acute metabolic effects of UCN2 were not mediated by SKM Gs signaling. Conclusions: Selective activation of Gs signaling in SKM causes an acute increase in blood glucose levels. However, acute in vivo stimulation of endogenous Gs-coupled receptors enriched in SKM has only a limited impact on whole-body glucose homeostasis, most likely due to the fact that these receptors are also expressed by pancreatic islets where they modulate insulin release. Read full article

HBx-induced cell cycle acceleration and the subsequent proliferative response via the induction of G1/S transcription factor 1; FBS: fetal bovine serum; GPCRs: G protein-coupled receptors; GST: glutathione S-transferase

Ho, ho, ho, GPCR elves! As the year wraps up, we're thrilled to present the final edition of the GPCR Weekly Newsletter for 2024! As researchers, we all understand the importance of data in driving meaningful discoveries  and advancing our experiments.   At Dr. GPCR, we believe the same principle applies to building a better experience  for our online community.   We’d love to hear your thoughts on our website and its features  so that we can continue to support your work and foster collaborations in the GPCR field.   Your feedback  will guide us in tailoring resources , tools , and content to meet your needs better and help fuel your research. Thank you for sharing your perspective and helping us shape the future of the Dr. GPCR ecosystem! Best, Yamina & the Dr. GPCR Team This Week’s Highlights: Congratulations to Andrew Tobin for an incredible week filled with prestigious events, including receiving the British Pharmacological Society Vane Medal and switching on the Christmas lights at the University of Glasgow Advanced Research Centre! Activation of the proton-sensing GPCR, GPR65 on fibroblast-like synoviocytes contributes to inflammatory joint pain Luke A Pattison , Rebecca H Rickman , Graham Ladds , Ewan St John Smith , et al. Attention, everyone! This is your last chance before the curtain closes: Classified GPCR News will be accessible only to VIP members next year! Indeed, all the details below will be limited to Premium Members . Don't miss out—upgrade now to keep up with your GPCR updates! Classified GPCR News  Let’s dive into the   Classified GPCR News from December 9th to 15th, 2024 Industry News When science meets serendipity: How accidental discoveries could revolutionise women’s health Seven unanswered questions about blockbuster weight-loss drugs Transforming Drug Discovery: Insights from Viva Biotech's GPCR and TPD Structural Biology Platforms GPCR Events, Meetings, and Webinars December 10 - 12, 2024 | Pharmacology 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery February 15 - 19, 2025 | BPS 2025 February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28, 2025 | 10th German Pharm-Tox Summit April 1 - 5, 2025 | XXIII GEM Meeting in 2025 April 3 - 6, 2025 | ASPET 2025 April 14 - 17, 2025 | 20th Drug Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15, 2025 | PEGS 2025 May 20 - 22, 2025 | SLAS Europe 2025 June 16 - 19, 2025 | BIO International Convention 2025 July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs GPCR Molecular Pharmacologist Scientist - Biology Scientist I Cell Biology - Tectonic Therapeutic Senior Principal Scientist, Medicinal Chemistry PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist GPCR Activation and Signaling Activation of the proton-sensing GPCR, GPR65 on fibroblast-like synoviocytes contributes to inflammatory joint pain Regulation of the chemokine receptors CXCR4 and ACKR3 by receptor activity-modifying proteins Single-cell transcriptomics of vomeronasal neuroepithelium reveals a differential endoplasmic reticulum environment amongst neuronal subtypes Methods & Updates in GPCR Research High-throughput optimisation of protein secretion in yeast via an engineered biosensor Optimized vector for functional expression of the human bitter taste receptor TAS2R14 in HEK293 cells Reviews, GPCRs, and more The role of the endocannabinoid system in the pathogenesis and treatment of epilepsy Become a Premium Member! Get your 5-day free trial TODAY!

S., Vojtek, M., Sousa, J. B., & Diniz, C. (2021). , S. K., Karnik, S. S., Hunyady, L., Luttrell, L. M., & Lefkowitz, R. J. (2003). , Volpe, S., Werthmann, R. A., Sriram, K., Wiley, S.

., Odongo, S., Radwanska, M., & Magez, S. (2023). pharmacology and toxicology, 57, 19–37. https://doi.org/10.1146/annurev-pharmtox-010716-104710 Rasmussen, S. S., Devree, B. T., Rosenbaum, D. M., Thian, F. S., Kobilka, T. S., Schnapp, A., Konetzki, I., Sunahara, R. K., Gellman, S. H., Pautsch, A., Steyaert, J., Weis, W. S., Ingram, J. R., Venkatakrishnan, A. J., Jude, K. M., Dukkipati, A., Feinberg, E.

., & Kongsamut, S. (2013). Minireview: targeting GPCR activated ERK pathways for drug discovery. Wei, H., Ahn, S., Shenoy, S. K., Karnik, S. S., Hunyady, L., Luttrell, L. M., & Lefkowitz, R.

Agonist activation of the β2-adrenoceptor (β2AR) causes its S-nitrosylation that is required for the Eliminating β2AR S-nitrosylation by mutation of C265 augments β2AR protein kinase A signaling, enables

S. (2002) National Human Genome Research Institute. S., Caron, M. G., Lefkowitz, R. J., & Strader, C. D. (1986). Molecular pharmacology, 63(6), 1256–1272. https://doi.org/10.1124/mol.63.6.1256 Syed Haneef, S. ., & Ranganathan, S. (2019). Structural bioinformatics analysis of variants on GPCR function.

Notably, the Y320F mutation restored some signaling capabilities, emphasizing Tyr320's role in membrane Reference Roy, S., Sinha, S., Silas, A. J., Ghassemian, M., Kufareva, I., & Ghosh, P. (2024).

First, we switched GPCRs between S. pombe and the closely related species Schizosaccharomyces octosporus , which showed that SoMam2 (Mam2 of S. octosporus) is partially functional in S. pombe, whereas SoMap3 (Map3 of S. octosporus) is not interchangeable.

signaling, they also influence specific pathways such as MAPK signaling (Song, X. et al. 2009, Coffa, S. S. F et al. 2021, Chen, H. et al. 2022). point of origin, suggesting the formation of active "nano domains" in specific membrane niches (Anton, S. S. et al. 2022). S. F. et al. 2021).

TRPM3's best understood function is its role as a peripheral noxious heat sensor in mice. However, a clear picture is needed to unravel TRPM3's full potential as experimental tool, diagnostic

while maintaining the responsiveness of canonical G protein-coupled CKRs that bind to the same ligand(s) example of a dual-function receptor that directly regulates both cell migration and scavenging (Volpe S.

., Trumpp-Kallmeyer, S., & Humblet, C. (1998). B., Chang, B., & Peisajovich, S. G. (2017). M., & Fields, S. (2014). Deep mutational scanning: a new style of protein science.

August 2022 "Aims: The pathophysiological mechanism(s) underlying non-alcoholic fatty liver disease (

., O'Brien, S. L., Stepniewski, T. K., Selent, J., Hill, S. J., & Calebiro, D. (2023). M., Kawakami, K., Masureel, M., Maeda, S., Garcia, K. C., von Zastrow, M., Inoue, A., & Kobilka, B. Reiter, E., Ahn, S., Shukla, A.K., and Lefkowitz, R.J. (2012).

This study examines these concerns by comparing AF2's predictions with experimental structures for docking This validates AF2's potential in enhancing drug discovery precision and efficiency.

express multiple ORs, tumor cells associated with the nervous system express a single OR gene type (Kalra S. Al 2017) and its activation promotes migration and angiogenesis (Kim S. et. al 2015). OR2AT4 activation leads to reduced proliferation and enhanced apoptosis of acute myeloid leukemia cells (S cells proliferation via activation by β-ionone which initiates prostate cancer cell cycle arrest (Jones S.

However, GRK3’s functions and clinical utility in GAC progression and metastases are unknown.

the responsiveness of canonical G protein–coupled chemokine receptors that bind to the same ligand(s) an example of a dual-function receptor that directly regulates both cell migration and scavenging (S. Grundmann et al. 2018), did not affect chemokine scavenging, consistent with prior work (S. Scavenging may allow cells to continuously migrate by remaining responsive to chemokines (S.

Previously, we had identified a novel pyrazole-based agonist 1 ((S)-N-(1-(cyclobutylamino)-1-oxo-5-(piperidin

Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5391-3. doi: 10.1073/pnas.90.12.5391. Faouzi A, Varga BR, Majumdar S. Biased Opioid Ligands. Shiraki A, Shimizu S.

November 2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, but Omass Therapeutics Ltd.’s

includes congrats to: Clementine E Philibert and Mikel Garcia-Marcos for their work on Smooth operator(s) challenges Modulating Vertebrate Physiology by Genomic Fine-Tuning of GPCR Functions Smooth operator(s)