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Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR reported as follows: (a) elderly (74-87 years at diagnosis), (b) male, (c) unexpectedly showed no other autoimmune diseases, (d) showed spontaneously fluctuating Ca levels from approximately normal to near fatally high

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

Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases "The chemokine receptor CXCR3 is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies, in particular autoimmune diseases.

., (NASDAQ: CCXI), a biopharmaceutical company focused on orally administered therapeutics to treat autoimmune diseases, inflammatory disorders and cancer, today announced that the companies have entered into a

monoclonal antibodies for the treatment of cancer, infections, metabolic disorders or inflammatory diseases Recently, functional autoantibodies targeting GPCRs have been associated with various disease-specific is to bring together the current knowledge on the role of autoantibodies targeting GPCRs in various diseases , such as cardiovascular diseases, renal diseases, autoimmune diseases such as systemic sclerosis or

September 2022 "Systemic sclerosis (SSc) is a systemic autoimmune disease with the key features of inflammation Extracellular vesicles are another novel player to possess disease processes.

targeted to 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

and it participates in inflammatory and immune responses that have been found to mediate apoptosis in autoimmune disease. β-arrestin2 and provided an experimental foundation for β-arrestin2 depletion in the treatment of the human autoimmune

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.

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

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

as sensory perception, reproduction, development, growth, metabolism, and are also linked to major diseases , such as neuroinflammatory, metabolic and autoimmune diseases. GPR84 has been additionally proposed to be a potential biomarker in different inflammatory diseases ( GPR84 is a promising target to exploit and the investment in better tools to study its function in both disease

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),

agonists Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases MRGPRX4 mediates phospho-drug-associated pruritus in a humanized mouse model GPCRs in Cardiology

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

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

Promising preclinical data supports the applicability of CB2 activation in autoimmune and inflammatory diseases, pain, neurodegeneration, and osteoporosis.

Promising preclinical data support the applicability of CB2 activation in autoimmune and inflammatory diseases, pain, neurodegeneration, and osteoporosis.

The chemokine receptor system is implicated in a wide range of inflammatory, autoimmune and infectious diseases (Proudfoot 2002), and in recent years attention has increasingly focused on cancer, where tumors a single receptor as patients cannot be stratified into CKRs specific subpopulations for a specific disease the majority of potential therapeutic applications are situated in the area of chronic inflammatory disease