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

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

Physiology Study In Anesthesiology Neurocrine Biosciences discovers new muscarinic M4 receptor antagonists Alexander S. Hauser on receiving 4.8 mill DKK from Carlsberg Foundation’s Semper Ardens: Accelerate programme.

Tanoli ,  Saad Hassan , Umut Onur Özcan ,   Jimmy Caroli ,   Albert J Kooistra ,   David E Gloriam ,   Alexander S Hauser GPCRdb in 2025: adding odorant receptors, data mapper, structure similarity search and models Pharmacology Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser

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

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

Nicole (Nicki) Perry-Hauser is now available What a fun chat! 📹Would you like to see the video?

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

s Check out the details of each course below: Open to the Public: Enrollment is Now Available! This week's highlight includes congrats to: Miles Thompson ,   Alexander Hauser ,   Caroline Gorvin ,

This week's highlight includes congrats to: Miles Thompson , Alexander Hauser , Caroline Gorvin ,   et

Miles Thompson, Alexander Hauser, Caroline Gorvin et al. for their research on GPCR gene variants and

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). emphasizing their role as hubs for increasing local effector concentrations near active GPCRs (Perry-Hauser S. et al. 2022). S. F. et al. 2021).

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.

efforts aim to accelerate drug discovery and improve clinical success Agreement to utilize Exscientia ’s develop up to 15 novel small molecule candidates across oncology and immunology, leveraging Exscientia ’s The companies have been working together since 2016 and in 2019, Sanofi in-licensed Exscientia ’s novel

HIGHLIGHT Research Associate - Professor Graeme Milligan HIGHLIGHT Postdoc in Molecular Pharmacology - The Hauser Natural Products and Compounds: Potential Therapeutic Targets for the Treatment of Neurological Disease s

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

as one of the most tractable classes of drug targets and are targeted by 30%–40% of current drugs (Hauser

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.

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

., Tectonic ’s SVP, Head of Research.

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 (