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August 2022 "Psychedelic research across different disciplines and biological levels is growing at a remarkably fast pace. In the prospect of a psychedelic drug becoming again an approved treatment, much of these efforts have been oriented toward exploring the relationship between the actual psychedelic effects and those manifestations of therapeutic interest. Considering the central role of the serotonin 5-HT2A receptor in the distinct effects of psychedelics in human psyche, neuropharmacology sits at the center of this debate and exploratory continuum. Here we discuss some of the most recent findings in human studies and contextualize them considering previous preclinical models studying phenomena related to synaptic plasticity. A special emphasis is placed on knowledge gaps, challenges, and limitations to evaluate the underpinnings of psychedelics' potential antidepressant action." Read more at the source #DrGPCR #GPCR #IndustryNews

In addition, the molecular mechanisms underlying GPCR-induced post-translational signaling regulation Here, we find that protease-activated receptor 4 (PAR4) unexpectedly acts as a potent oncogene, inducing the N-terminal portion of β-catenin suppresses the ubiquitination of β-catenin, thereby promoting PAR-induced Taken together, we reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally

September 2022 "The endocannabinoid system plays a key role in the intersection of the nervous, endocrine, and immune systems, regulating not only their functions but also how they interplay with each other. Endogenous ligands, named endocannabinoids, are produced “on demand” to finely regulate the synthesis and secretion of hormones and neurotransmitters, as well as to regulate the production of cytokines and other proinflammatory mediators. It is well known that immune challenges, such as exposure to lipopolysaccharide, the main component of the Gram-negative bacteria cell wall, disrupt not only the hypothalamic–pituitary–adrenal axis but also affects other endocrine systems such as the hypothalamic–pituitary–gonadal axis and the release of oxytocin from the neurohypophysis. Here we explore which actors and molecular mechanisms are involved in these processes." Read more at the source #DrGPCR #GPCR #IndustryNews

Our results indicate that lateral diffusion parameters of serotonin1A receptors in normal cells are consistent Notably, our results show that statin-induced dynamic confinement could be reversed by destabilization

October 2022 Activation of GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity Here, we show that 7α,25-OHC-induced behavioral hypersensitivity is Gα i dependent, but not β-arrestin In support, we found that the development of 7α,25-OHC/GPR183-induced mechano-allodynia was associated Intrathecal injections of the GPR183 agonist 7α,25-OHC induce behavioral hypersensitivity, and these We found that 7α,25-OHC-induced allodynia is dependent on MAPK and NF-κB signaling pathways and results

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid

September 2022 Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal In the present work, we explored the molecular basis of cholesterol-induced thermal stability of the

studies in experimental animals have shown that certain subsets of T cells express functional GLP-1R, indicating activated under T helper (Th) 1, Th2, Th17 and regulatory T (Treg) cell differentiation conditions indicated that GLP-1R expression was most pronounced in induced Treg (iTreg) cells. Given the high induction of GLP-1R in human iTreg cells, we hypothesize that GLP-1R+ iTreg cells play

Evidence is also indicated to demonstrate that PLC activities self-regulate the expression of PLC isozymes

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in We further found that cAMP/PKA signalling promotes Brd4 recruitment to dopamine-induced genes in striatal neurons, and that knockdown of Brd4 attenuates D1R-induced gene expression.

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

Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic

Our previous study indicated that ARBB1 (arrestin beta 1) promotes hepatocellular carcinogenesis (HCC Arrb1 deficiency suppressed HBx-induced hepatocellular carcinogenesis in several mouse models. Furthermore, knockdown of ARRB1 blocked HBx-induced macroautophagic/autophagic flux and disrupted the Inhibition of autophagy by 3-methyladenine or interference of ATG5 or ATG7 attenuated HBx-induced cell B virus; HBx: hepatitis B virus X protein; HMGB1: high mobility group box 1; HIF1A/HIF-1α: hypoxia inducible

Join us for the first virtual cafe talk to hear about the amazing work that Dr. Brian Arey is doing. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

August 2022 "GPCRs in Medicinal Chemistry Event 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry

Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine receptor CXCR4 WHIM syndrome is a rare immunodeficiency disorder that is characterized by warts, hypogammaglobulinemia Here, we report on a new WHIM syndrome mutation that results in a frame shift within the codon for Ser339 S339fs5) and compare the properties of S339fs5 with wild type CXCR4 and a previously identified WHIM syndrome Taken together, these studies identify a new WHIM syndrome mutant, CXCR4-S339fs5, that promotes enhanced

March 2022 Inversago Pharma Announces Dosing of First Participant with Metabolic Syndrome in Phase 1B portfolio of CB1 inverse agonists, announced today the dosing of the first participant with metabolic syndrome pharmacokinetics and safety profile of Inversago’s lead molecule, INV-202, on a targeted population with metabolic syndrome

of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in primary Sjögren's syndrome The etiology of primary Sjögren's syndrome (pSS) remains unknown, and there is no ideal drug for the In this study, we established an experimental Sjögren's syndrome (ESS) mouse model to elucidate the molecular results showed that IFNα activated GRP78-ATF6-CHOP apoptosis signaling, decreased cell viability, and induced apoptosis signaling is involved in the pathogenesis of pSS and that β-arrestin2 encourages inflammation-induced

August 2022 "The X-linked form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism

disease implications GPCRs in Oncology and Immunology LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced transcriptomic analysis reveals complex neuroendocrine regulatory networks mediated by spinal cord injury-induced immunodeficiency G protein-coupled receptors: A target for microbial metabolites and a mechanistic link

chemokine receptor 5 (CCR5), a major receptor in inflammation and the principal entry co-receptor for Human Immunodeficiency

September 2022 "Background Spinal cord injury (SCI) is a common trauma in clinical practices. Subacute SCI is mainly characterized by neuronal apoptosis, axonal demyelination, Wallerian degeneration been discovered in recent years that inflammatory responses are particularly important in subacute SCI The models of the three gene expression profiles were all for SCI to the thoracic segment of the rat.

Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5391-3. doi: 10.1073/pnas.90.12.5391. Complex Persistent Opioid Dependence-an Opioid-induced Chronic Pain Syndrome.

Ya Zhuo , Joseph Crecelius , Sara Benzow , Adriano Marchese Cannabinoid regulation of angiotensin II-induced announces the positive results of its clinical Phase 1/2 Study with AEF0217 in young adults with Down syndrome Mechanistic Insights Into Redox Damage of the Podocyte in Hypertension Endurance exercise attenuates Gαq-RNAi induced novel regulator of Aβ42 production in Alzheimer's disease Cannabinoid regulation of angiotensin II-induced dynamics GPCRs in Oncology and Immunology Gallein, G protein βγ subunits inhibitor, suppresses the TGF-α-induced

., Agonist-induced formation of unproductive receptor-G(12) complexes.  Proc Natl Acad Sci U S A, 2020. 117(35): p. 21723-21730. 2.     

Proc Natl Acad Sci U S A, 2012. 109 (45): p. 18607-12. 8.          ., Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1 induces G-protein-coupled

We found that some agonist-induced GPCR/14-3-3 signal intensities can rapidly decrease. We confirmed that this phenomenon of rapidly decreasing agonist-induced GPCR/14-3-3 signal intensity could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal

transactivation of EGF and TGF-β receptors in phosphorylation of Smad2L and protein expression of PAI-1 induced <br /><strong>Results:</strong> TGF (2 ng/ml), EGF (100 ng/ml) and ET-1 (100 nM) induced the phosphorylation <br /><strong>Conclusion:</strong> The results indicated that ET-1 increases the phosphorylation of Smad2L and protein expression of PAI-1<br />via induced the transactivation pathways of EGFR and TGFR.