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March 2022 "Congratulations to Richard J. Law, our newly named Chief Business Officer. Richard is the architect behind nearly all of Exscientia's partnerships and collaborations across pharma

June 2022 "CRN04894 Selected for Oral Presentation SAN DIEGO, June 8, 2022 — Crinetics Pharmaceuticals and other conditions driven by excess adrenocorticotropic hormone (ACTH), were selected for an oral presentation

October 2022 "The prefrontal cortex (PFC) is a hub for cognitive control, and dopamine profoundly influences

October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though as yet unrealised, therapeutic potential. Promising preclinical data supports the applicability of CB2 activation in autoimmune and inflammatory diseases, pain, neurodegeneration, and osteoporosis. A diverse pharmacopoeia of cannabinoid ligands is available, which has led to considerable advancements in the understanding of CB2 function and extensive preclinical evaluation. However, until recently, most CB2 ligands were highly lipophilic and as such not optimal for clinical application due to unfavourable physicochemical properties. A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties and a few such compounds have now undergone clinical trial. We review the current state of CB2 ligand development and progress in optimising physicochemical properties, understanding advanced molecular pharmacology such as functional selectivity, and clinical evaluation of CB2-targeting compounds." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though as yet unrealized, therapeutic potential. Promising preclinical data support the applicability of CB2 activation in autoimmune and inflammatory diseases, pain, neurodegeneration, and osteoporosis. A diverse pharmacopeia of cannabinoid ligands is available, which has led to considerable advancements in the understanding of CB2 function and extensive preclinical evaluation. However, until recently, most CB2 ligands were highly lipophilic and as such, not optimal for clinical application due to unfavorable physicochemical properties. A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties and a few such compounds have now undergone clinical trials. We review the current state of CB2 ligand development and progress in optimizing physicochemical properties, understanding advanced molecular pharmacology such as functional selectivity, and clinical evaluation of CB2-targeting compounds." Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital (Nasdaq: NBIX) today announced that it will present new Phase 2 data on the use of crinecerfont in adolescent These data will be shared as an oral presentation by Ron S. ET (Presentation #OR18) at ENDO 2022, the Endocrine Society's 104th annual meeting in Atlanta from June The company also presented data highlighting patient preferences and treatment patterns in classic CAH

Surprisingly, phosphorylation of the RGS promotes completion of cytokinesis before pheromone-induced Completion of cytokinesis in the presence of pheromone is promoted by the kelch-repeat protein, Kel1 These data lead us to a model where Kel1 promotes completion of cytokinesis before pheromone-induced

October 2022 Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent epithelial-neutrophil signaling via the defensin-Mrgpra2 axis in maintaining healthy skin ecology and promoting

August 2022 "Aims: The pathophysiological mechanism(s) underlying non-alcoholic fatty liver disease (NAFLD) have yet to be fully delineated and only a single drug, peroxisome proliferator-activated receptor (PPAR) α/γ agonist saroglitazar, has been approved. Here, we sought to investigate the role of Regulator of G Protein Signaling 7 (RGS7) in hyperlipidemia-dependent hepatic dysfunction. " Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand CCL25 to promote

September 2022 GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome properties in colonic macrophages through enhancing NLRP3 inflammasome activation, while the loss of GPR84 prevents

signaling via the GPCRs, β2-adrenergic receptor (β2AR), and metabotropic glutamate receptor 2 (mGluR2) promotes destabilizing microtubules and impeding p62/SQSTM1 autophagy flux by interfering with p62 body formation, which promotes

Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial Infarction Their remote myocardia showed increased mRNA and protein levels of collagen I/III with higher levels Conclusion: Exendin-4 inhibits the remodeling in the remote myocardium of rats following acute MI by graphical abstract that illustrates the mechanisms by which Exendin-4 inhibits cardiac remodeling in remote stimulate PP2A to dephosphorylation Smad3 (inhibition) and GSK3β (activation), thus reduces fibrosis and prevents

September 2022 "The transparency of the cornea along with its dense sensory innervation and resident leukocyte populations make it an ideal tissue to study interactions between the nervous and immune systems. The cornea is the most densely innervated tissue of the body and possesses both immune and vascular privilege, in part due to its unique repertoire of resident immune cells. Corneal nerves produce various neuropeptides that have a wide range of functions on immune cells. As research in this area expands, further insights are made into the role of neuropeptides and their immunomodulatory functions in the healthy and diseased cornea. Much remains to be known regarding the details of neuropeptide signaling and how it contributes to pathophysiology, which is likely due to complex interactions among neuropeptides, receptor isoform-specific signaling events, and the inflammatory microenvironment in disease. However, progress in this area has led to an increase in studies that have begun modulating neuropeptide activity for the treatment of corneal diseases with promising results, necessitating the need for a comprehensive review of the literature. This review focuses on the role of neuropeptides in maintaining the homeostasis of the ocular surface, alterations in disease settings, and the possible therapeutic potential of targeting these systems." Read more at the source #DrGPCR #GPCR #IndustryNews

Premont, R. T. & Gainetdinov, R. R.

Therefore, the presentation of 10 or more Nobel prizes highlights the importance of research work on GPCRs mediated signal transduction.[47] The 2000 Nobel Prize in Physiology or Medicine went to Eric Richard The 2004 Nobel Prize in Physiology or Medicine went to Richard Axel and Linda Brown Buck for their work Press release: The 2004 Nobel Prize in Physiology or Medicine to Richard Axel and Linda B. Richard Axel – Facts - NobelPrize.org. https://www.nobelprize.org/prizes/medicine/2004/axel/facts/. 61

PVT NPSR1 neurons recruit the nucleus accumbens shell and structures in the prefrontal cortex and amygdala

agonist targeting neurological and psychiatric disorders: An in silico approach Opioid modulation of prefrontal cortex cells and circuits GPCRs in Oncology and Immunology RGS20 promotes non-small cell lung carcinoma receptors that bind cry toxins of Bacillus thuringiensis Industry News Domain Therapeutics announces the promotion

succinate response in people with prediabetes GPCRs in Neuroscience Spatiotemporal organization of prefrontal Operational Highlights and Consolidated Results for the First Quarter 2024 Crinetics Pharmaceuticals To Present