Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs The experimental structure of these receptors has yet to be determined, and key-residues controlling relationships and proposes functional molecular switches that encode agonist sensing and downstream signaling

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while in the role of GPCRs in lifespan are those that mimic dietary restriction, those related to insulin 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 a Gq coupled receptor. These data support a model where Gq and Gβγ-dependent signaling cooperatively regulate PLC activation

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Proton-sensing G-protein coupled receptors are activated by acidic environments, but their role in fibrosis Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in We demonstrate that OGR1 protein expression is significantly reduced in lung tissue from patients with We then demonstrate that sub-cellular localization and alternative signaling pathways may be responsible

The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different subtypes of S1P receptors Several S1PR therapeutic drugs have been developed to treat these diseases; however, they lack receptor In this article, we describe a 2.2 Å resolution room temperature crystal structure of the human S1P5 receptor demonstrates a unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies the receptor

Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor (GPCR) GPR183 Further investigation of the signaling pathways downstream of GPR183 is needed to support the development Our findings provide novel mechanistic insight into how GPR183 signaling in the spinal cord produces We found that 7α,25-OHC-induced allodynia is dependent on MAPK and NF-κB signaling pathways and results This study provides a first insight into how GPR183 signaling in the spinal cord is pronociceptive."

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 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

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 coupled receptors (GPCRs). , very few studies have focused on the stringency of pheromone receptors. both in the intracellular regions that regulate the downstream signaling of pheromones and in the activation

Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled receptors expressed in tumors G protein-coupled receptors (GPCRs) are the largest family of human proteins. They have a common structure and, signaling through a much smaller set of G proteins, arrestins, and Because there are many more GPCRs than effectors, mutations in different receptors could perturb signaling These data suggest that recurrent impactful oncogenic mutations perturb different GPCRs to subvert signaling

GABAB receptors inhibit Ca2+ entry, whereas 5-HT1B receptors target SNARE complexes. We demonstrate in male and female rats that GABAB receptors receptors alter Pr, whereas 5-HT1B receptors 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. alteration on Ca2+ and the effect of this altered Ca2+ signal on 5-HT1B receptor signaling.

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that

October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system In the former, stimulation of Gs-coupled receptors leads to increases in contractility, whereas stimulation of Gq-coupled receptors modulates cellular survival and hypertrophic responses. We also review the hierarchy of signaling events driving the fibrotic response and the communications We discuss how such events may be distinct depending on where the GPCRs and their associated signaling

September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor Cryo-electron microscopy studies revealed a drastic conformational change upon activation and a unique G protein (GP) binding mode. However, little is known about the mechanism for GP coupling and activation for class C GPCRs.

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 IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate of component signalling pathways for in vivo M33 function.

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

Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are

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

Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic analysis and review Odorant receptors (ORs) account for about 60% of all human G protein-coupled receptors

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

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.

Regulator G protein Signaling (RGS) proteins are critical components of the intracellular signaling pathways that mediate the effects of G protein-coupled receptors (GPCRs). protein that is coupled to the receptor and leading to a decrease in dopamine signaling[4, 5]. Senese, N.B., et al., Regulator of G-Protein Signaling (RGS) Protein Modulation of Opioid Receptor Signaling Wang, D., The essential role of G protein-coupled receptor (GPCR) signaling in regulating T cell immunity

These findings shed light on a sophisticated signaling network directed by intestinal microbial metabolites

November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies inhibitory GAIN domain and the dipping of the cleaved stalk peptide into the ligand-binding pocket of receptors A comparison of Gq, Gs, Gi, and G12 engagements with ADGRL3 reveals the key determinant of G-protein coupling on the far end of αH5 of Gα. Taken together, our study lays the groundwork for understanding aGPCR activation and G-protein-coupling

coupling and mediate intracellular pathway bias "Within the intestine, the human G protein-coupled receptor (GPCR) GPR35 is involved in oncogenic signaling, bacterial infections, and inflammatory bowel disease cells to thoroughly profile both GPR35 isoforms for constitutive and ligand-induced activation and signaling of 10 different heterotrimeric G proteins, ligand-induced arrestin recruitment, and receptor internalization Our results reveal that the extended N-terminus of the long isoform limits G protein activation yet elevates

conformational consequences of the differential activity of cannabidiol with two endocannabinoid-activated G-protein-coupled receptors "Cannabidiol (CBD), the major non-psychoactive phytocannabinoid present in the plant Cannabis belong to the family of G-protein-coupled receptors (GPCRs). investigate the interacting determinants of CBD in two closely related endocannabinoid-activated GPCRs, the G-protein-coupled receptor 55 (GPR55) and the cannabinoid type 1 receptor (CB1).

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors How this HR is involved in hormone binding and signal transduction is still an open question. The models are expected to allow for testable hypotheses about signal transduction and drug development

October 2022 Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in mGlu5a receptor internalization "The internalization of G protein-coupled receptors (GPCRs) can be regulated by PKC. containing a mutated putative adaptor protein complex 2 (AP-2) interaction motif, we demonstrate that internalization of rat mGlu5a is mediated by Gαq/11 proteins (77% of the response), GRK2 (27%), and

2022 Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors "Neural network (NN)-based protein modeling methods have improved significantly in recent G-protein-coupled receptor (GPCR) proteins are particularly interesting since they are involved in numerous This work directly compares the performance of these novel deep learning-based protein modeling methods We collected the experimentally determined structures of 73 GPCRs from the Protein Data Bank.