Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Many cause receptor misfolding and failure to reach the cell surface. We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone receptors

Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion of mesenchymal Chemokines are low molecular weight proteins that their functional activities are achieved by binding to the cell surface G protein-coupled receptors (GPCRs). Chemokine and chemokine receptors are of the most important and effective molecules in MSC trafficking Chemokine/chemokine receptor axes play a pivotal role in the recruitment and oriented trafficking of

September 2022 Identification and functional characterization of the sulfakinin and sulfakinin receptor As a neuromodulator, it mediates a variety of behavioral processes and physiological functions in invertebrates through the interaction with G-protein-coupled receptors (GPCRs).

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous However, the activation profiles of the GPR15 receptor within Gi/o subtypes have not been examined. Gα protein signalling using a G protein activation assay and second messenger assay conducted on living Within the Gi/o family, the GPR15 receptor activates all the subtypes (Gi1 , Gi2 , Gi3 , GoA , GoB and and the activation rate is significantly slower.

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early (Daphnia magna) reveals a high level of orthological relationship of amine, neuropeptide, and opsin receptor repertoire, while purinergic and chemokine receptors were highly differentiated in humans. Our findings suggest sporadic evolutionary processes within the GPCR gene families identified in D. celebensis

September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous carcinoma: an emerging prognostic indicator and future therapeutic target "Purpose: Beta 2-Adrenergic Receptor Immunohistochemistry, western blot and quantitative real-time PCR techniques were used to analyze β2-AR protein

September 2022 Sweet taste receptor agonists attenuate macrophage IL‐1β expression and eosinophilic inflammation Trehalose is a disaccharide sugar with known pro‐autophagy activity and effective in alleviating diverse were assessed using specific inhibitor, genetic knockdown or knockout, and overexpression of cognate receptors

September 2022 "Given the promising clinical value of allosteric modulators of G protein-coupled-receptors Here, we report the crystallographic and cryo-electron microscopy structures of the cannabinoid receptor ZCZ011 exerts a PAM effect by promoting TM2 rearrangement in favor of receptor activation and increasing the population of receptors that adopt an active conformation.

September 2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS -7 cells transfected with their cognate receptor "Results of previous studies provided evidence for the CRE-luc activity in COS-7 cells transfected with their cognate receptor GnIHR. Notably, GnIH2 antagonized Kiss2-evoked CRE-luc activity in COS-7 cells expressing GnIHR and Kiss2 receptor However, GnIH peptides did not alter NFAT-RE-luc activity and ERK phosphorylation levels.

October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz Previous assays verified that a typical G protein-coupled receptor, β-adrenergic-like octopamine receptor

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated 2 (ICL2) and the C terminus of APH1A, which differentially regulate recruitment of the scaffolding protein domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin complex, which regulates γ-secretase activity

October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental G protein-coupled receptors, the largest family of membrane proteins in eukaryotes and the largest drug Among them, the secretin/adhesion (Class B) G protein-coupled receptors are essential drug targets for Given the great value of the secretin/adhesion (Class B) G protein-coupled receptors in the regulation of cardiovascular system function and the drug target exploration, we summarize the role of these receptors

Understanding real-time kinetics to predict activity and in vivo target coverage. Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position GPCR Activation and Signaling Preassembly of specific Gβγ subunits at GABAB receptors through auxiliary KCTD proteins of Group I Metabotropic Glutamate Receptors Dual regulation of IP3 receptors by IP3 and PIP2 controls 1 in zebrafish Coupling and Activation of the β1 Adrenergic Receptor - The Role of the Third Intracellular

the cytoskeleton and lipid microdomains in controlling signalling compartmentalization during T cell activation , we discuss mechanisms responsible for signalling amplification and compartmentalization in T cell activation , focusing on the role of CD28, chemokine receptors and the actin cytoskeleton. We also take into account the detrimental effect of mutations carried by distinct signalling proteins

October 2022 "Psychedelics, also known as classical hallucinogens, affect processes related to perception , cognition and sensory processing mostly via the serotonin 5-HT2A receptor (5-HT2AR).

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while maintaining good health since they have a substantial participation in a wide variety of processes of In this way, we present the analysis of a series of GPCRs whose activity has been shown to affect the

September 2022 β2-Adrenergic Receptor Expression and Intracellular Signaling in B Cells Are Highly Dynamic In the past, treatment of arthritic B cells with a β2-adrenergic receptor (β2-ADR) agonist has been shown Splenic B cells were isolated via magnetic-activated cell sorting (MACS). Adrenergic receptors on B cells and intracellular β2-ADR downstream molecules (G protein-coupled receptor agonist terbutaline by flow cytometry. β2-ADR-expressing B cells increase during CIA without a change in receptor

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 activation. Ca2+ In combination these pathways allow complex presynaptic integration.SIGNIFICANCE STATEMENTTwo G protein Co-activation of these receptors allows synaptic integration because of convergence of GABAB receptor

Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall webworm Hyphantria cunea Background: Insect G protein-coupled receptors (GPCRs) have been identified as a new generation HLGR2 is a typical GPCR and shows high structural and sequence similarity with other insect LGR2 proteins

August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in A variety of ligands for CB1 receptors have been developed as promising drug candidates for the treatment our molecular understanding of CB1 ligand interactions, selectivity, receptor activation and allosteric In this review, we describe the structural determinants for modulation of CB1 receptors by different types of ligands, as well as the differences between CB1 and its homologous, the CB2 receptor.

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, A major pan-receptor focus has been to identify GPCR-selective ligands that have bias in G protein-dependent the past two decades, it is only recently that highly β-arrestin biased ligands for the dopamine D1 receptor

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. This mechanism provides fresh insights into the mechanistic details of class C GPCRs activation expected

kinase C isozymes are involved in mGlu5a receptor internalization "The internalization of G protein-coupled receptors (GPCRs) can be regulated by PKC. to investigate the contribution of PKC isozymes in the internalization of the metabotropic glutamate receptor Direct activation of PKC and mutation of rat mGlu5a Ser901, a PKC-dependent phosphorylation site in the receptor C-tail, both showed that PKC isozymes facilitate approximately 40% of the receptor internalization

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination coupled receptors (GPCRs). Although such pheromone/receptor systems are likely to function in both mate choice and prezygotic isolation , 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

Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, GPR110 belongs to adhesion GPCR and was the functional receptor of N-docosahexaenoyl ethanolamine (also Synaptamide suppressed osteoclastogenesis induced by receptor activator of nuclear factor-kappa B ligand

September 2022 "The G-protein-coupled bile acid receptor, Gpbar1 or TGR5, is characterized as a membrane receptor specifically activated by bile acids. extracellular regulated protein kinases (ERK1/2), signal transducer and activator of transcription 3 activated by cAMP (Epac), and transient receptor potential ankyrin subtype 1 protein (TRPA1) signaling recent studies have demonstrated that TGR5 exerts inconsistent effects in different cancer cells upon activating

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on We previously demonstrated that a reduction in extracellular pH activates latent TGF-β1, and that TGF-β1 then drives its own activation, creating a feed-forward mechanism that propagates myofibroblast differentiation 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

sympatholytic treatments (such as β-blockers) and renin-angiotensin system inhibitors or mineralocorticoid receptor 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. 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).