Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings there is emerging interest in defining if agonists of GPR84 might find utility in conditions in which regulation

Alberto Gonzalez-Hernandez, Hermany Munguba, Joshua Levitz for their work on Emerging modes of regulation of neuromodulatory G protein-coupled receptors Dr. GPCR Activation and Signaling Emerging modes of regulation of neuromodulatory G protein-coupled receptors of G protein signaling 6 (RGS6) in dopamine neurons promotes EtOH seeking, behavioral reward, and susceptibility suppress hormones GPCR Events, Meetings, and Webinars June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein

Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain 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

October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical

Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog) activates Rho1 signaling The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent

August 2022 Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP relationship between the conformational change of the receptor because of the mutation and related downstream signaling R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type receptor. between the changed conformation of the receptor and consequently activated signaling pathways, and

In the endosomes, sustained G protein signaling has been associated with prolonged interactions between and the spatial organization of signaling effectors, including G proteins, adenylyl cyclases, and kinases regulation of GPCR signaling and downstream responses1,2. signal-regulated kinases 1 and 2. Neurochemical research, 42(1), 166–172. https://doi.org/10.1007/s11064-016-2026-6 Mendizabal-Zubiaga,

Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog) activates Rho1 signaling The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent

September 2022 "GPCR signaling and function depend on their associated proteins and subcellular locations Besides G-proteins and β-arrestins, 14-3-3 proteins participate in GPCR trafficking and signaling, and they connect a large number of diverse proteins to form signaling networks. could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination type depends on the molecular recognition of two peptidyl mating pheromones by their corresponding G-protein and SoMap3, which revealed differences between the receptors both in the intracellular regions that regulate the downstream signaling of pheromones and in the activation by the pheromone.

Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic with GPR108 and promoted its degradation, knockout of GPR108 remarkably blocked GA inhibition of NF-κB signaling

One fascinating aspect of the cellular signaling network is the crosstalk between G protein-coupled receptors heterotrimeric G proteins. On the other hand, RTKs play pivotal roles in growth factor signaling, regulating cell growth, differentiation protein signaling? protein signaling in disease.

We now aim to determine the molecular mechanism by which this functional microbiome output regulates models, we confirmed the RNA sequencing findings and discovered a role for intestinal HNF4α in P-gp regulation These findings shed light on a sophisticated signaling network directed by intestinal microbial metabolites

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR) signaling The kinase GRK2 and the multifunctional scaffolding protein β-arrestin2 are key integrated signaling nodes in various biological processes, and both of them regulate cell proliferation and promote cell

the initial GPCR-G protein association step, ensuring precise downstream signalling activation. This unproductive coupling revealed that non-cognate G protein interactions could modulate GPCR signalling coupling efficiency of cognate G proteins to GPCRs, thereby amplifying canonical downstream signalling , facilitating subsequent coupling of cognate G proteins and promoting enhanced signalling. Gupte, T.M., et al., Priming GPCR signaling through the synergistic effect of two G proteins. 

The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo ) genomes analysed to date is the presence of G protein-coupled receptors (GPCR). Constitutive G protein-coupled M33 signalling is required for these phenotypes, although the contribution constitutively activate phospholipase C β (PLCβ) and downstream cyclic AMP response-element binding protein IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate

Chemical communication controls a wide range of behaviors via conserved signaling networks. We demonstrate that the chemoreceptor genes, srg-36 and srg-37 , which encode G protein-coupled receptors Therefore, the ascaroside signaling system provides a unique example of a signaling molecule that regulates SIGNIFICANCE STATEMENT In C. elegans , axon regeneration is positively regulated by the EGL-30 Gqα-JNK However, it remains unclear what signals activate the EGL-30 pathway in axon regeneration.

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle through their cognate G protein-coupled receptors (GPCR). Prolonged vasoconstrictor GPCR signalling increases arterial contraction and stimulates signalling pathways GPCR signalling through phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt) promotes VSMC proliferation In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled Receptor D Induces Release of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling G protein-coupled Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed However, involvement of the human Mas-related G-protein coupled receptor D (MRGPRD) in the regulation β-alanine-induced signaling through MRGPRD was investigated further by probing downstream signaling

Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled (GPCR) signaling systems leading to mitogenic signaling in PDAC cells.

November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies A comparison of Gq, Gs, Gi, and G12 engagements with ADGRL3 reveals the key determinant of G-protein Taken together, our study lays the groundwork for understanding aGPCR activation and G-protein-coupling

SIGNIFICANCE STATEMENT Two G protein coupled receptors colocalize at presynaptic sites, to mediate presynaptic We have investigated downstream effects of signaling and integrative properties of these receptors. integration because of convergence of GABAB receptor alteration on Ca2+ and the effect of this altered Ca2+ signal on 5-HT1B receptor signaling.

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs relationships and proposes functional molecular switches that encode agonist sensing and downstream signaling

August 2022 GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin protein-coupled receptors (GPCRs) through selective coupling of Gs, Gi, or Gq proteins. The structural basis for G protein subtype selectivity by these GPCRs remains elusive. We find that the macro-switch by the TM5-TM6 length is shared by class A GPCR-G protein structures. Together, these results present a common mechanism of Gs versus Gi protein coupling selectivity or promiscuity

October 2022 Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric dynamic fluxes in the 3D architecture of the receptors, as the basis of ligand selectivity, efficacy, and regulation

correlate with three cholesterol molecules that play essential roles in conformation stabilization and signaling Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor ) signaling and provide insights into the diversity of G protein coupling."

and anosmia, is due to mutations in the ANOS1 gene that encodes for the extracellular matrix (ECM) protein Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled current report we present evidence of the modulation of PK2/PKR2 activity by anosmin 1, since this protein is able to enhance the activation of the ERK1/2 (extracellular signal-regulated kinase 1/2) pathway The whey acidic protein domain (WAP) is necessary for this modulatory activity, although data from GST

Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of a great variety Like many other organs, various GPCRs play a role in regulating liver function. However, our knowledge of how GPCRs regulate liver metabolism and fibrosis in the different cell types better understanding of the role of GPCRs in hepatic stellate cells (HSCs), the primary cells that regulate