Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment of Non-Alcoholic Fatty Liver Disease The prevalence of non-alcoholic fatty liver disease (NAFLD) is Gaining control over disease-related events in non-alcoholic steatohepatitis (NASH), an advanced form

The present study aims to investigate the possible role of FSH excess in male bone health, by comparing

., 2017 ), including those lining bone marrow (BM) sinusoids ( Duchene et al., 2017 ).

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

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),

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

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

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

of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases Oncology and Immunology Wnt pathway inhibition with the porcupine inhibitor LGK974 decreases trabecular bone but not fibrosis in a murine model with fibrotic bone The orphan G protein-coupled receptor 141 expressed

We also review the hierarchy of signaling events driving the fibrotic response and the communications

as sensory perception, reproduction, development, growth, metabolism, and are also linked to major diseases , such as neuroinflammatory, metabolic and autoimmune diseases. immune cells in a range of pro‐inflammatory disorders renders it a promising target in inflammatory and fibrotic 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

We showed that cGAS expression was induced in fibrotic liver and kidney, but suppressed in endothelial

) ligands and analogues for their pharmacologic activities and potential therapeutic utility toward diseases of bone and mineral ion metabolism. responses to injected PTH analog peptides that are consistent with a fully functional human PTH1R in target bone

multiple sclerosis patients Multiple sclerosis (MS) is a specific type of chronic immune-mediated disease Despite intensive research, a known treatment for MS disease yet to be introduced. Thus, the development of novel and safe medications needs to be considered for the disease management MSCs have several sources and they can be derived from the umbilical cord, adipose tissue, and bone marrow

October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical seven transmembrane (TM) helix architecture. Recent advances in X-ray crystallography and cryo-EM have resulted in a wealth of GPCR structures that have been used in drug design and formed the basis for mechanistic activation hypotheses. Here, ensemble refinement (ER) of crystallographic structures is applied to explore the impact of binding of agonists and antagonist/inverse agonists to selected structures of cannabinoid receptor 1 (CB1R), β2 adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source #DrGPCR #GPCR #IndustryNews

Sir William Osler Scientists have long sought to discover a “golden bullet” that would cure every disease The more we know about the pathology of diseases, the more complicated it is to modulate them by a specific Extracellular Signal-Regulated Kinase: A Regulator of Cell Growth, Inflammation, Chondrocyte and Bone