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Regulator G protein Signaling (RGS) proteins are critical components of the intracellular signaling pathways As negative regulators of GPCR signaling, RGS proteins play a critical role in regulating the duration ., Regulator of G-Protein Signaling (RGS) Protein Modulation of Opioid Receptor Signaling as a Potential Hepler, Cellular regulation of RGS proteins: modulators and integrators of G protein signaling. ., The essential role of G protein-coupled receptor (GPCR) signaling in regulating T cell immunity.

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 Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer."

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias proper cardiac output and circulation, is regulated by G protein-coupled receptor (GPCR) signaling. Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause G protein dysregulation, contributing to modest blood pressure elevation and exaggerated cardiac hypertrophic Whether RGS2 and 5 redundantly control G protein signaling to maintain cardiovascular homeostasis is

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 The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 genes coding for these proteins.

The mammalian target of rapamycin (mTOR) senses upstream stimuli to regulate numerous cellular functions Understanding the upstream regulators of mTORC1 will provide a crucial link to targeting mTORC1 hyperactivated In this review, we will discuss the regulation of mTORC1 by upstream stimuli, with a specific focus on G-protein coupled receptor (GPCR) signaling to mTORC1. Significance Statement mTORC1 is a master regulator of many cellular processes and is often hyperactivated

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein protein signaling. We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease glial response that may limit amyloid plaque development in G protein-biased GPR3 AD mice. Collectively, these studies indicate that GPR3-mediated G protein and β-arrestin signaling produce discrete

October 2022 "Enzymatic and cellular signalling biosensors are used to decipher the activities of complex Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in Their applications have continually expanded our understanding of this important protein class. selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric signalling

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR ) signaling pathway because of its quantifiable stimulus, non-redundancy of genes, and immense importance published cryo-electron tomography (cryo-ET) data on the ROS with structural knowledge on individual proteins reconstruction of the rod phototransduction system highlights the potential roles of phosphodiesterase 6 maintaining the spacing between ROS discs, suggesting a plausible mechanism by which intrinsic optical signals

October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance 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

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor ability for growth hormone (GH) release to reduce wasting in aging individuals, as well as food intake regulation Known roles of GHSR1a now extend to regulation of neurogenesis, learning and memory, gastrointestinal In vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors This review discusses the signalling mechanisms of GHSR1a alone and in combination with other GPCRs,

October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway PKA facilitates the actions of hormones, neurotransmitters and other signaling molecules that bind G-protein Through its control of synaptic events, exocytosis, transcriptional regulation, and more, PKA signaling regulates cellular metabolism and emotional and stress responses making it integral in the maintenance Neural PKA signaling is regulated by afferent and peripheral efferent signals that link specific neural

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Simulations and Quantum Chemical Calculations "Allosteric modulators are called promising candidates in G protein-coupled receptor (GPCR) drug development by displaying subtype selectivity and more specific

October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular signaling pathways. YM-254890 (YM) can inhibit signaling by both GPCR-activated wild type αq and GPCR-independent αqQ209L Treatment of cells with YM failed to inhibit signaling by these PM-restricted αqQ209L. both αqQ209L and PM-restricted αqQ209L, resulting in increased binding to βγ and decreased binding to regulator

October 2022 "Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled This review will focus in particular on pepducins designed from protease-activated receptors, C-X-C motif discuss the historic context of pepducin development for each receptor, as well as the structural, signaling

August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases, bound to these interaction partners available today do not reveal a clear conformational basis for signaling

Intracellular calcium ([Ca2+]i) signaling is a critical regulator of chondrogenesis, chondrocyte differentiation Calcium (Ca2+) signaling is known to direct processes that govern chondrocyte gene expression, protein Synthetic signaling platforms permitting precise and selective Ca2+ signal transduction can improve dissection dynamics, proliferation, and protein deposition in 2D ATDC5 cultures. This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

Most acquired genes are transmembrane proteins and cytokines, such as viral G protein-coupled receptors (vGPCRs), chemokines, and chemokine-binding proteins. from human cytomegalovirus, which encodes four vGPCRs: US27, US28, UL33, and UL78; human herpesvirus 6 We discuss ligand binding, signaling, and structures of the vGPCRs in light of robust differences from

September 2022 "Heterotrimeric G-protein transducin, Gt, is a key signal transducer and amplifier in The only other farnesylated G-protein γ-subunit, Gγ11 (Gng11), is expressed in multiple tissues but not To determine whether Gγ1 regulates uniquely rod phototransduction, we generated transgenic rods expressing

October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid Deletion of phospholipase Cβ3 (PLCβ3), or selective inhibition of Gβγ regulation of PLCβ3, enhances the 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 Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of Adhesion Receptor GPR97 "Adhesion G-protein-coupled receptors (aGPCRs)-a major family of GPCRs-play critical roles in the regulation of tissue development and cancer progression. Our study provides mechanistic insights into the regulation of aGPCRs via post-translational modifications of the Go protein, and offers guidance for future drug design of aGPCRs."

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis "β-Arrestins are ubiquitously expressed intracellular proteins with many functions now recognized that in addition to GPCR arresting (hence the name arrestin). β-Arrestins are 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.

September 2022 GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization However, its regulating signaling pathways remain to be elucidated. We investigated the influence of specific inhibitors of G protein-coupled receptors (GPCR), endocytosis pathways, extracellular signal-regulated kinases 1/2 (ERK1/2) signaling, p38 signaling, mitochondrial 97 (TMEM97)—a recently identified target protein of Hst1.

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous GPR15 signals through the Gi/o pathway to decrease intracellular cyclic adenosine 3',5'-monophosphate GPR15L(71-81) are used as pharmacological tool compounds to delineate the GPR15 receptor-mediated Gα protein signalling using a G protein activation assay and second messenger assay conducted on living cells. Furthermore, the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked

Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling (LYCHOS, previously annotated as G protein-coupled receptor 155), a multidomain transmembrane protein that enables cholesterol-dependent activation of the master growth regulator, the protein kinase mechanistic concentrations, LYCHOS bound to the GATOR1 complex, a guanosine triphosphatase (GTPase)-activating protein pathway for cholesterol sensing and couples cholesterol concentrations to mTORC1-dependent anabolic signaling

Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine The S339fs5 and R334X mutants exhibited significantly increased signaling compared to wild type CXCR4 including agonist-promoted calcium flux and extracellular signal-regulated kinase activation. together, these studies identify a new WHIM syndrome mutant, CXCR4-S339fs5, that promotes enhanced signaling phosphorylation, β-arrestin binding and endocytosis, and a very high basal rate of degradation that is not protected

Historically, drug discovery efforts targeting GPCRs focused on G-protein-dependent signaling pathways signaling, are now recognised as critical players in activating extracellular signal-regulated kinases Extracellular signal-regulated kinases (ERK), a subset of the mitogen-activated protein kinase (MAPK) Extracellular Signal-Regulated Kinase: A Regulator of Cell Growth, Inflammation, Chondrocyte and Bone signal-regulated kinases 1 and 2.

September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its N-terminal fragment 1 to 36 "The parathyroid hormone (PTH)-related protein (PTHrP) is indispensable through its cognate G-protein coupled receptor (GPCR), the PTH type 1 receptor (PTHR), is largely derived Furthermore, we show that the molecular basis for biased signaling differences between PTHrP1-36 and native protein hormone acting in conjunction with a GPCR."

receptor-transducer 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 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