greater understanding of how effector molecules interact with a receptor to initiate downstream effector signaling This review aims to explore the signaling pathways, dynamic structures, and physiological relevance in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins is increasing appreciation for the elegance of the regulatory mechanisms that mediate intracellular signaling

GPR15 signals through the Gi/o pathway to decrease intracellular cyclic adenosine 3',5'-monophosphate (cAMP). -81) are used as pharmacological tool compounds to delineate the GPR15 receptor-mediated Gα protein signalling Furthermore, the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked

A finely tuned signalling compartmentalization orchestrated in dynamic platforms is an essential requirement several studies have depicted the pivotal role of the cytoskeleton and lipid microdomains in controlling signalling Here, we discuss mechanisms responsible for signalling amplification and compartmentalization in T cell We also take into account the detrimental effect of mutations carried by distinct signalling proteins

Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling pathway for cholesterol sensing and couples cholesterol concentrations to mTORC1-dependent anabolic signaling

September 2022 β2-Adrenergic Receptor Expression and Intracellular Signaling in B Cells Are Highly Dynamic In this study, the expression and signaling of β2-ADR in B cells during collagen-induced arthritis (CIA 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 The change of β2-ADR expression and signaling during sustained inflammation might be an integral part

October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the

October 2022 Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric

GPCRs show great diversity in their intracellular location, interacting partners and effectors, and signaling Here we will discuss recent studies on the diversity of location, effectors, and signaling of GPCRs, and how these could interact to generate specific spatiotemporal patterns of GPCR signaling in cells.

September 2022 GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization However, its regulating signaling pathways remain to be elucidated. influence of specific inhibitors of G protein-coupled receptors (GPCR), endocytosis pathways, extracellular signal-regulated kinases 1/2 (ERK1/2) signaling, p38 signaling, mitochondrial respiration and Na+/K+-ATPase activity Overall, phagocytosis, CME, GPCR, ERK signaling, and S2R/TMEM97 are involved in the internalization of

encode a variety of bioactive small molecules with growing evidence for N-acyl amides as being important signaling Both groups of metabolites suppress anti-inflammatory interleukin-10 signaling in human macrophage cell

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer which interact directly and indirectly with a wide number of cellular partners and mediate downstream signaling adaptor proteins that control the recruitment, activation, and scaffolding of numerous cytoplasmic signaling complexes and assist in G-protein receptor signaling, thus bringing them into close proximity. This review delivers a concise overview of the role of β-arrestins with a primary emphasis on the signaling

October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid Here we investigated a potential mechanism for regulation of PLC signaling downstream of MOR in HEK293 cells and found that MOR alone could not stimulate PLC, but rather required a coincident signal from These data support a model where Gq and Gβγ-dependent signaling cooperatively regulate PLC activation

October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture

discuss the historic context of pepducin development for each receptor, as well as the structural, signaling

GPCR function has revealed new paradigms with increasingly complex models of receptor activation and signaling Spatial-temporal signaling of GPCRs and physiological functions; 2. The structural basis for GPCR activation of down-stream signaling and regulatory proteins; and 4.

Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein or β-arrestin signaling Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling Our previous work demonstrated that GPR3-mediated β-arrestin signaling modulates amyloid-β (Aβ) generation reduced fertility, and memory impairment, which are potentially associated with impaired G protein signaling We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR) signaling maintaining the spacing between ROS discs, suggesting a plausible mechanism by which intrinsic optical signals

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer Information flow from a source to a receiver becomes informative when the recipient can process the signal Information exchange and interpretation is essential in biology and understanding how cells integrate signals communication occurs mostly through neurotransmitters and hormones, and receptors are responsible for signal led to the hypothesis that their dimeric state can provide the framework for temporal coincidence in signaling

with GPR108 and promoted its degradation, knockout of GPR108 remarkably blocked GA inhibition of NF-κB signaling

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer which interact directly and indirectly with a wide number of cellular partners and mediate downstream signaling adaptor proteins that control the recruitment, activation, and scaffolding of numerous cytoplasmic signaling complexes and assist in G-protein receptor signaling, thus bringing them into close proximity. This review delivers a concise overview of the role of β-arrestins with a primary emphasis on the signaling

GPCR Symposium on GPCR Activation and Signaling held on May 19th, 2023. GPCR Activation and Signaling Phosphorylation barcodes direct biased chemokine signaling at CXCR3. SUCNR1 signaling in adipocytes controls energy metabolism by modulating circadian clock and leptin expression Local 5-HT signaling bi-directionally regulates the coincidence time window for associative learning. GPCR-mediated calcium and cAMP signaling determines psychosocial stress susceptibility and resiliency

GPCR Activation and Signaling The G protein alpha chaperone and guanine-nucleotide exchange factor RIC and their ligand from the tick Ixodes scapularis Evidence that pyrophosphate acts as an extracellular signalling Optical Approaches for Investigating Neuromodulation and G Protein-Coupled Receptor Signaling Protocol G-protein-coupled receptors Reviews, GPCRs, and more RGS proteins and cardiovascular Angiotensin II Signaling signaling revealed AI Predicts How GPCRs Respond to Drug-Like Molecules Accurately predicting GPCR P2Y1

September 2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS Herein, we further elucidated the intracellular signaling pathways mediating in sea bass GnIH actions and the potential interactions with sea bass kisspeptin (Kiss) signaling. GnIH can interfere with kisspeptin actions by reducing its signaling. Our results provide additional evidence for the understanding of signaling pathways activated by GnIH

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling cystadenocarcinoma: p = 0.048); (d) RGS20 was found to be significantly associated with some tumor-related signaling

Robert Lefkowitz for their work on GPCRs: from radioligand binding to cellular signaling Dr. Next week, on March 15th, we are hosting a symposium on GPCR activation and signaling. State-dependent dynamics of extramembrane domains in the β2 -adrenergic receptor β-Arrestin-independent endosomal cAMP signaling by a polypeptide hormone GPCR Bias translation: The final frontier? Bicarbonate signalling via G protein-coupled receptor regulates ischaemia-reperfusion injury GPCRs in

Furthermore, in sPD models, the shortening of PC is accompanied by increased Sonic Hedgehog (SHH) signal Inhibiting overactive SHH signaling may be a potential neuroprotective therapy for sPD."

Matthew Eddy and lab research on GPCR signaling mechanisms using NMR spectroscopy with labeled receptors GPCR Activation and Signaling The non-nutritive sweetener sucralose increases β-arrestin signaling at the constitutively active orphan G protein-coupled receptor GPR52 β-Arrestin-independent endosomal cAMP signaling by a polypeptide hormone GPCR Gαs is dispensable for β-arrestin coupling but dictates GRK of the fish taste receptor type 1 (T1R) family by the extracellular chloride ion Illuminating GPCR signaling

., for their study on   Systems modeling of oncogenic G-protein and GPCR signaling reveals unexpected , location bias, signaling bias). Let’s dive into the   Classified GPCR News  from July 15th to 21st, 2024 GPCR Activation and Signaling maintains muscle stem cell quiescence and prevents stem cell loss Activation of Polycystin-1 Signaling formation: Implications for obesity and metabolic health GPCRs in Neuroscience Chronic modulation of cAMP