Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial Infarction Purpose: This study tested if the protective anti-remodeling effect of GLP-1 agonist Exendin-4 after an acute Conclusion: Exendin-4 inhibits the remodeling in the remote myocardium of rats following acute MI by

Objective: The goal of this study was to determine the glucometabolic effects of acute activation of expressed by SKM at relatively high levels (β2-adrenergic receptor and CRF2 receptor) and studied the acute Results: Acute stimulation of GsD signaling in SKM impaired glucose tolerance in lean and obese mice The acute metabolic effects following agonist activation of β2-adrenergic and, potentially, CRF2 receptors The acute metabolic effects of UCN2 were not mediated by SKM Gs signaling.

use disorder GPCRs in Oncology and Immunology Regulator of G protein signaling protein 6 alleviates acute lung injury by inhibiting inflammation and promoting cell self-renewal in mice Methods & Updates in

September 2022 "Background Spinal cord injury (SCI) is a common trauma in clinical practices.

However, the potential role of GPR3 in axonal regeneration after neuronal injury has not been elucidated investigated retinal GPR3 expression and its possible involvement in axonal regeneration after retinal injury

October 2022 Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the iterative optimization of a chemical series culminating in the discovery of the selective CXCR3 antagonist ACT In a LPS-induced lung inflammation model in mice, ACT-660602 led to significantly reduced recruitment

Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild traumatic brain injury "Traumatic brain injury (TBI) is a leading cause of disability in the US. Angiotensin 1-7 (Ang-1-7), an endogenous peptide, acts at the G protein coupled MAS1 receptors (MASR) This study examined the therapeutic effect of Ang-(1-7) on secondary injury observed in a murine model of mild TBI (mTBI) in a closed skull, single injury model."

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs be an important factor for survival in four other cancers (clear renal cell carcinoma: p < 0.001, lung ; (d) RGS20 was found to be significantly associated with some tumor-related signaling pathways and long

Juan Jose Fung, Principal Scientist, at GPCR Therapeutics.

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. Despite considerable advances in pharmacological treatment, HF represents a severe clinical and social burden. Chronic human HF is characterized by several important neurohormonal perturbations, emanating from both the autonomic nervous system and the adrenal glands. Circulating catecholamines (norepinephrine and epinephrine) and aldosterone elevations are among the salient alterations that confer significant hormonal burden on the already compromised function of the failing heart. This is why sympatholytic treatments (such as β-blockers) and renin-angiotensin system inhibitors or mineralocorticoid receptor antagonists, which block the effects of angiotensin II (AngII) and aldosterone on the failing heart, are part of the mainstay HF pharmacotherapy presently. The adrenal gland plays an important role in the modulation of cardiac neurohormonal stress because it is the source of almost all aldosterone, of all epinephrine, and of a significant amount of norepinephrine reaching the failing myocardium from the blood circulation. Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs), such as adrenergic receptors and AngII receptors. In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain to modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR types in that context, adrenergic receptors and AngII receptors (AT 1 Rs). Particular emphasis is given to findings from the past decade and a half that highlight the emerging roles of the GPCR-kinases and the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs in all tissues, including the myocardium and the adrenal gland." Read more at the source #DrGPCR #GPCR #IndustryNews

The data support the inference that they act at the active interface between both transmembrane domains developing allosteric compounds able to specifically modulate the activity of GPCR homo- and heterodimers by acting

-1 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 GPCR-Targeted Biologic Trevena Announces Acceptance of Abstract Examining the Use of OLINVYK in Patients with Acute Burn Injuries Carmot Therapeutics Enters into Definitive Merger Agreement with Roche New Clinical Trial

receptor is stabilized by TSH ligand Cardiomyocyte-specific overexpression of GPR22 ameliorates cardiac injury in mice with acute myocardial infarction GPCRs in Neuroscience Voltage tunes mGlu5 receptor function $4.6 Million in Milestone Payments from Centessa Pharmaceuticals CB1 receptor inverse agonist improves lung

from receptor trafficking GPCR Binders, Drugs, and more An inverse agonist of orphan receptor GPR61 acts human islets AT2 receptor agonist LP2 restores respiratory function in a rat model of bleomycin-induced lung G protein-coupled receptor 37 promotes resistance to cisplatin-induced apoptosis in non-small cell lung after securing separate AI drug discovery deals with Merck KGaA Pfizer’s Vydura recommended by NICE for acute

Pulmonary Fibrosis "Idiopathic pulmonary fibrosis (IPF) is a disease characterized by irreversible lung pathophysiology is not fully understood, but the working hypothesis postulates that a combination of epithelial injury We demonstrate that OGR1 protein expression is significantly reduced in lung tissue from patients with

analyses, have indicated that OR genes are also expressed in non-olfactory tissues including the testis, lung myelogenous leukemia where OR2AT4 activation leads to reduced proliferation and enhanced apoptosis of acute In non-small-cell lung cancer OR2J3 activation induced apoptosis and inhibited cell proliferation and migration in long-term stimulus experiments (Kalbe B. et al. 2017).

Finally, we briefly discuss the therapeutic targeting of vGPCRs as future treatment of acute and chronic

One potential solution is to develop analgesics that act at targets other than opioid receptors. Experimental approach: We used a series of behavioural assays to evaluate the acute responses of mice

GPCRs, we utilized single particle tracking (SPT) to monitor diffusion of serotonin1A receptors under acute

GPCRs, we utilized single particle tracking (SPT) to monitor diffusion of serotonin1A receptors under acute

The fact that GPR84 expression in leukocytes is remarkably increased under acute inflammatory stimuli

FFAR4 improves the senescence of tubular epithelial cells by AMPK/SirT3 signaling in acute kidney injury Research CPGL: Prediction of Compound-Protein Interaction by Integrating Graph Attention Network With Long

showed spontaneously fluctuating Ca levels from approximately normal to near fatally high ranges, (e) acute

context-dependent compared to the C5aR1, which has received enormous attention for its role in both acute

the United States by the Food and Drug Administration (FDA) for use in adults for the management of acute

Hello GPCR Enthusiasts, Dive into this week's exciting updates on cutting-edge GPCR research, new learning But act fast – this offer is only available for a limited time. Not a premium member yet? downregulation GPCRs in Cardiology, Endocrinology, and Taste Role of G protein coupled receptors in acute kidney injury Ligand-Dependent and G Protein-Dependent Properties for the Sweet Taste Heterodimer, TAS1R2 pain and chronic inflammation Developmental exposures to common environmental pollutants result in long-term

Check out our latest collection of 25 cutting-edge research papers on GPCRs and exciting updates on industry for their investigation on Modulation of contextual fear acquisition and extinction by acute and chronic GPCR Event Highlight Immerse yourself in the cutting-edge world of adhesion GPCR research at the highly expression and signaling in murine brain tissue Modulation of contextual fear acquisition and extinction by acute

Although PTHrP1-36 induces transient cAMP production, acute intracellular Ca2+ (iCa2+) release and β-arrestin results contribute to a better understanding of the biased signaling process of a native protein hormone acting