Until recently, itch pathophysiology was poorly understood and treatments were poorly effective in relieving itch. Current progress in our knowledge of the itch processing, the numerous mediators and receptors involved has led to a large variety of possible therapeutic pathways. Currently, inhibitors of IL-31, IL-4/13, NK1 receptors, opioids and cannabinoids, JAK, PDE4 or TRP are the main compounds involved in clinical trials. However, many new targets, such as Mas-related GPCRs and unexpected new pathways need to be also explored. Read full article

October 2022 "Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing Despite a better understanding of the disease, the current mainstay of treatment cannot modify pathogenesis suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets for Alzheimer's disease In this review, we provide an accessible summary of the literature on Alzheimer's disease and the therapeutic

August 2022 "Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing prevalence Despite a better understanding of the disease, the current mainstay of treatment cannot modify pathogenesis suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets for Alzheimer's disease In this review, we provide an accessible summary of the literature on Alzheimer's disease and the therapeutic

August 2022 "Cardiovascular diseases (CVDs) represent the leading cause of death globally.

April 2022 "By Sophie Bradley | Apr 12, 2022 Summary Sophie Bradley, Translational Sciences Associate Director at Sosei Heptares , recently presented at the Keystone Symposia GPCR Conference, a summary of work performed both at Sosei Heptares and Glasgow University characterizing the role of the muscarinic M1 receptor in cognitive and neurodegenerative disorders and the potential therapeutic benefit of muscarinic M1 selective ligands." Read more at the source #DrGPCR #GPCR #IndustryNews

chemotaxis of leukocytes, especially neutrophils, during inflammation, a key process in cardiovascular disease

chemotaxis of leukocytes, especially neutrophils, during inflammation, a key process in cardiovascular disease

autophagy deficiency in myeloid cells "Background Eosinophilic inflammation is a hallmark of refractory chronic disaccharide sugar with known pro‐autophagy activity and effective in alleviating diverse inflammatory diseases

normal glutamate transmission has been implicated in a variety of neurodegenerative and neuropsychiatric diseases contribution of mGluR2 and mGluR3 to the pathophysiology of some neurodegenerative and neuropsychiatric diseases including Amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, Parkinson's diseases

October 2022 Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone Peptide-Derived diabetes (T2DM) is provoking an important socioeconomic burden mainly in the form of cardiovascular disease

September 2022 "Parkinson’s disease (PD) as a progressive neurodegenerative disorder arises from multiple

pathways, are leading to the development of drugs with superior efficacy and reduced side effects in heart disease Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD),

focused on the discovery, development and commercialization of novel therapeutics for rare endocrine diseases

Positive Phase 3 Data for KINECT-HD Study Evaluating Valbenazine for Chorea Associated with Huntington Disease Statistically Significant Reduction in Chorea Movements (p < 0.0001) as Measured by the Unified Huntington's Disease inhibitor being investigated as a once-daily treatment in adults with chorea associated with Huntington disease met the primary endpoint of reduction in severity of chorea, the cardinal motor feature in Huntington disease , as measured by change in the Unified Huntington's Disease Rating Scale (UHDRS®) Total Maximal Chorea

Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators for rare diseases

Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR follows: (a) elderly (74-87 years at diagnosis), (b) male, (c) unexpectedly showed no other autoimmune diseases

lipopolysaccharide (LPS) and TNFα suggests that it may play a role in the development of inflammatory and fibrotic diseases

September 2022 β2-Adrenergic Receptor Expression and Intracellular Signaling in B Cells Are Highly Dynamic during Collagen-Induced Arthritis "The sympathetic nervous system (SNS) has either a pro-inflammatory or anti-inflammatory effect, depending on the stage of arthritis. In the past, treatment of arthritic B cells with a β2-adrenergic receptor (β2-ADR) agonist has been shown to attenuate arthritis. In this study, the expression and signaling of β2-ADR in B cells during collagen-induced arthritis (CIA) were investigated to provide an explanation of why only B cells from arthritic mice are able to improve CIA. Splenic B cells were isolated via magnetic-activated cell sorting (MACS). Adrenergic receptors on B cells and intracellular β2-ADR downstream molecules (G protein-coupled receptor kinase 2 (GRK-2), β-Arrestin 2, p38 MAPK, extracellular signal-regulated kinase 1/2 (ERK1/2) and cAMP response element-binding protein (CREB)) were analyzed at different time points in naïve and arthritic B cells with and without stimulation of β2-ADR agonist terbutaline by flow cytometry. β2-ADR-expressing B cells increase during CIA without a change in receptor density. Moreover, we observed a profound downregulation of GRK-2 shortly after induction of arthritis and an increase in β-Arrestin 2 only at late stage of arthritis. The second messengers studied (p38, ERK1/2 and CREB) followed a biphasic course, characterized by a reduction at onset and an increase in established arthritis. Stimulation of CIA B cells with the β-ADR agonist terbutaline increased pp38 MAPK independent of the timepoint, while pERK1/2 and pCREB were enhanced only in the late phase of arthritis. The phosphorylation of p38 MAPK, ERK1/2 and CREB in the late phase of arthritis was associated with increased IL-10 produced by B10 cells. The change of β2-ADR expression and signaling during sustained inflammation might be an integral part of the switch from pro- to anti-inflammatory action of sympathetic mechanisms in late arthritis." Read more at the source #DrGPCR #GPCR #IndustryNews

new antifibrotic cGAS/STING signaling pathway that suppresses pathological angiogenesis in liver and kidney We showed that cGAS expression was induced in fibrotic liver and kidney, but suppressed in endothelial cells. cGAS genetic deletion promoted liver and kidney fibrosis and pathological angiogenesis, including GPCR)-based antagonist that blocks the profibrotic activity of endothelial YAP, attenuated liver and kidney Further, pharmacological targeting of cGAS/STING-YAP axis exhibits the potential to alleviate liver and kidney

Adhesion GPCRs Adhesion G Protein-Coupled Receptor Gpr126 (Adgrg6) Expression Profiling in Diseased Mouse , Rat, and Human Kidneys GPCR Activation and Signaling Differential regulation of G protein-coupled receptor-associated proteins in the caudate and the putamen of cynomolgus macaques following chronic ethanol drinking GRK5

October 2022 "Systolic heart failure (HF) is a chronic clinical syndrome characterized by the reduction in cardiac function and still remains the disease with the highest mortality worldwide. Chronic human HF is characterized by several important neurohormonal perturbations, emanating from both GPCR signaling and regulation, as they pertain to modulation of cardiac function in the context of chronic

clinical-stage global biopharmaceutical company developing novel oral therapeutics to treat a wide range of chronic diseases, today introduced Basecamp Bio, a wholly owned subsidiary dedicated to fueling ShouTi ’s pipeline

revealed by 19F NMR spectroscopy Role of protease activated receptor 4 (PAR4) in mouse models of acute and chronic kidney injury GPCR Binders, Drugs, and more High-throughput virtual screening of potential inhibitors of GPR52 using docking and biased sampling method for Huntington's disease therapy Rational design of

) ligands and analogues for their pharmacologic activities and potential therapeutic utility toward diseases injected PTH analog peptides that are consistent with a fully functional human PTH1R in target bone and kidney

modulate inflammatory responses, offering potential therapeutic avenues for conditions such as autoimmune diseases and chronic inflammation. exploring the roles of these receptors in various pathological states, including cancer and infectious diseases

downregulation GPCRs in Cardiology, Endocrinology, and Taste Role of G protein coupled receptors in acute kidney GPCR-Mediated Natural Products and Compounds: Potential Therapeutic Targets for the Treatment of Neurological Disease s Activation of GPR55 alleviates neuropathic pain and chronic inflammation Developmental exposures to

Molecular Endocrinology and Pharmacology Laboratory team who are investigating new ways to tackle the disease-inducing chronic inflammation that is linked to type 2 diabetes."