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

Juan Jose Fung, Principal Scientist, at GPCR Therapeutics.

Brian Krumm and Bryan Roth studied CryoEM structures of adhesion in GPCR CD97, filling gaps. receptor negatively modulates substance P responses by forming complex with Neurokinin-1 receptor NTR-1's

Bryan Roth There are 10 open tickets available. Get yours now!

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

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.

odorant molecules which initiate a neuronal response that drives odorant discrimination and perception (Young analyses, have indicated that OR genes are also expressed in non-olfactory tissues including the testis, lung 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). In non-small-cell lung cancer OR2J3 activation induced apoptosis and inhibited cell proliferation and

Bryan Roth and Brian Krumm   for their study on Molecular glues as potential GPCR therapeutics Drs

Bryan Roth, Peter Gmeiner, and Thomas P. Sakmar this week. For Dr. patients with WHIM syndrome Bristol Myers Squibb’s Investigational LPA1 Antagonist Reduces the Rate of Lung

., & 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

Bryan L Roth study on Illuminating the understudied GPCR-ome Save the dates: February 8 - 29: Dr. disorder GPCRs in Oncology and Immunology Regulator of G protein signaling protein 6 alleviates acute lung

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

CUB domain of the adhesion GPCR ADGRG6/GPR126 is a key regulator of receptor signaling Jiankun Lyu, Brian Shoichet, Bryan Roth, et al. for their research on AlphaFold2 structures guide prospective ligand discovery

Katharina Grotsch, Bryan L Roth, Valery V Fokin  et al. for their research on Virtual Screening of a Frizzleds act as dynamic pharmacological entities Marina Casiraghi, Robert J Lefkowitz, Peter Gmeiner, Brian

fantastic paper on Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor Bryan Roth  and Brian Krumm  for their excellent study on Molecular glues as potential GPCR therapeutics Sabrina

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).

Bryan Roth, Sudarshan Rajagopal, and Graeme Milligan. Save the date! Dr.

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

., Tectonic ’s SVP, Head of Research.