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 modulation by Gβγ, but one - a GABAB receptor inhibits Ca2+ entry while another - a 5-HT1B receptor competes with Ca2+-synaptotagmin binding to the synaptic vesicle machinery. GABAB receptors alter Pr leaving synaptic properties unchanged, while 5-HT1B receptors fundamentally

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while

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).

September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination the molecular recognition of two peptidyl mating pheromones by their corresponding G-protein coupled receptors 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. GPCRs might reflect the significantly distinct stringency/flexibility of their respective pheromone/receptor

September 2022 A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under we show for the first time that MRP3 expression is induced under hypoxia through the A2B adenosine receptor Downregulation of the A2B receptor decreases MRP3 expression and chemosensibilizes GSCs treated with These data suggest that hypoxia-dependent activation of A2B adenosine receptor promotes survival of GSCs

September 2022 Interacting binding insights and conformational consequences of the differential activity 55 (GPR55) and the cannabinoid type 1 receptor (CB1). In addition, our results suggest a previously unknown sodium-binding site located in the extracellular domain of the CB1 receptor. From our detailed characterization, we found particular interacting loci in the binding sites of the

neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor Co-immunoprecipitation and pull-down assays confirmed interaction between NFα1/CPE and 5-HTR1E and 125I NF-α1/CPE-binding studies demonstrated saturable, high-affinity binding to 5-HTR1E in stably transfected HEK293 cells (ICL3) of NF-α1/CPE-5-HTR1E, it recruited β-arrestin1 by forming numerous salt bridges and hydrogen bonds Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB

by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells transfected with their cognate receptor significantly decreased forskolin-elicited CRE-luc activity in COS-7 cells transfected with their cognate receptor Notably, GnIH2 antagonized Kiss2-evoked CRE-luc activity in COS-7 cells expressing GnIHR and Kiss2 receptor

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

August 2022 "The atypical chemokine receptor 1 (ACKR1) was discovered on erythrocytes as the Duffy blood group antigen ( Cutbush et al., 1950 ), also called Duffy-antigen/receptor for chemokines, or DARC ( In light of the extensive literature, these findings have been particularly provocative, as this was

) that cause nephrogenic diabetes insipidus "Loss-of-function mutations of the arginine vasopressin receptor AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP Investigation into the characterization of biased receptors may give insights into the 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.

Mitogen-Activated Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor Our findings provide novel mechanistic insight into how GPR183 signaling in the spinal cord produces

Numerous physiological effects of melatonin are mediated via its specific G protein-coupled receptors (GPCRs) named the MT1 receptor, which couples to both Gq and Gi proteins, and the MT2 receptor, which We investigated whether melatonin receptors are expressed on airway smooth muscle; whether they regulate Activation of melatonin MT2 receptors with either pharmacological concentrations of melatonin (10-100 These findings suggest that the melatonin MT2 receptor is expressed in ASM, and modulates airway smooth

binding by searching large-scale motions accompanied with stable maintenance of the fragile cell-membrane Then sampling was conducted from conformations where bosentan was distant from the binding site in the hETB binding pocket. The following binding mechanism was inferred. Last, in the pocket, ligand–receptor attractive native contacts are formed.

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

The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo Common to all cytomegalovirus (CMV) genomes analysed to date is the presence of G protein-coupled receptors Gq/11 to constitutively activate phospholipase C β (PLCβ) and downstream cyclic AMP response-element binding IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate

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 A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology We recently reported the initial characterization of a NanoBRET-based conformational histamine H3 receptor H3R biosensor in membrane preparations and found that observed potency values better correlated with binding affinity values that were measured in radioligand competition binding assays on membranes. conformational biosensor in membranes might be a ready-to-use, high-throughput alternative for radioligand binding

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle circulation of vasoconstrictors, resulting in enhanced signalling through their cognate G protein-coupled receptors In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

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

Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β -Arrestin Interaction These receptors are the most clinically productive drug targets at present. components of receptor-effector interactions remain incompletely described. The β 2-adrenergic receptor ( β 2AR) is a prototypical and extensively studied GPCR that can provide with G protein and β-arrestin with a biased loss of β-arrestin binding.

G protein-coupled receptors (GPCRs) are major drug targets, yet their complex and dynamic structures on structure-based ligand discovery remained uncertain due to the necessity for accurately modeled binding Docking 490 million molecules against the σ2 receptor's AF2 model yielded a 54% hit rate, comparable Functional activity of selected compounds was assessed across 5-HT2A, 5-HT2B, and 5-HT2C receptors, with binding.

proteomes, we identified lysosomal cholesterol signaling (LYCHOS, previously annotated as G protein-coupled receptor

September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer coupling and mediate intracellular pathway bias "Within the intestine, the human G protein-coupled receptor activation and signaling of 10 different heterotrimeric G proteins, ligand-induced arrestin recruitment, and receptor results reveal that the extended N-terminus of the long isoform limits G protein activation yet elevates receptor-β-arrestin contributed by the extended N-terminus of the long GPR35 isoform limits the extent of agonist-induced receptor-β-arrestin2

2022 N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 receptor selectivity towards more GLP-1 receptor interaction "Background and purpose: To fully elucidate the regulatory role of the GLP-2 system in the gut and the bones, potent and selective GLP-2 receptor (GLP COS-7 cells were transfected with the human GLP-2R and assessed for cAMP accumulation or competition binding To examine selectivity, COS-7 cells expressing human GLP-1 or GIP receptors were assessed for cAMP accumulation

on the mechanism of signal activation, ligand selectivity and allosteric modulation in angiotensin receptors Thus, we need to know much more about the structures of receptor-ligand complexes at high resolution. Recently, X-ray structures of both AngII receptors (AT1 and AT2 receptors) bound to peptide and non-peptide , as the basis of ligand selectivity, efficacy, and regulation of the molecular functions of the receptors This review covers the new data elucidating the structural dynamics of AngII receptors and how structural