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

follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled 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 "Protease activated receptors (PARs) are among the first receptors shown to transactivate We will discuss recent evidence as well as what we consider as emerging areas to explore; from the signalling relevance of these interactions, since this additional level of molecular cross-talk between receptors and signaling

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 We collected the experimentally determined structures of 73 GPCRs from the Protein Data Bank. smallest average modeling RMSD of 2.17 Å, which is better than AlphaFold's 5.53 Å and RoseTTAFold's 6.28

G protein-coupled receptors (GPCRs) are membrane-bound proteins that sense external stimuli and relay SecR dimerization enhances the receptor’s signaling efficiency by increasing its dynamics in a G protein-dependent manner [6]. Bouvier, M., Oligomerization of G-protein-coupled transmitter receptors.   Pharmacol Rev, 2016. 68 (4): p. 954-1013. 6.         

October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR smoothened "The oncogenic G-protein-coupled receptor (GPCR) Smoothened This effect involves the sequential and additive action of protein kinase A, casein kinase I, and the morphogenetic effects of HH to the apico-basal distribution of SMO and provide a novel mechanism for the regulation

October 2022 "Background: Uncoupling proteins (UCPs) are unpaired electron carriers that uncouple oxygen hypothesised to be triggered by superoxide and then reduce mitochondrial free radical production, potentially protecting Objectives: The objectives of the study are to find out the newest ways to treat diabetes mellitus through protein

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 transcriptomic analysis, mutational profiles revealed that somatic mutations in OR genes were detected in ＞ 60% [BMB Reports 2021; 54(12): 601-607]. Read full article

August 2022 "The common mechanisms by which members of the G protein-coupled receptor (GPCR) family respond GPCRs show great diversity in their intracellular location, interacting partners and effectors, and signaling Here we will discuss recent studies on the diversity of location, effectors, and signaling of GPCRs, and how these could interact to generate specific spatiotemporal patterns of GPCR signaling in cells.

counting techniques enable a precise determination of the intracellular abundance and stoichiometry of proteins Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical on the potential for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor signaling."

applications of Nbs to facilitate the development of more selective drugs capable of modulating specific signaling Potential for protein crystallization: Nanobodies can be used to stabilize the protomers of larger protein International journal of molecular sciences, 24(6), 5994. https://doi.org/10.3390/ijms24065994 Manglik Nanobodies to Study G Protein-Coupled Receptor Structure and Function. Structural basis for chemokine recognition and activation of a viral G protein-coupled receptor.

Opioid receptors belong to class A of G protein-coupled receptors or GPCRs and signaled mainly through that have addressed the differences in the mechanisms of transduction triggered by MOR, reporting that G-protein This report highlights a mechanism of β-arrestin pathway activation dependent on G protein activation These findings highlight how G proteins and β-arrestins are involved in driving intracellular signaling The molecular associations in clathrin-coated pit regulate β-arrestin-mediated MAPK signaling downstream

October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture pathways that have not been previously implicated in Hc interaction with macrophages, including the ragulator complex (involved in nutrient stress sensing), glycosylation enzymes, protein degradation machinery, The highest scoring protective hits included the complement C3a receptor (C3aR), a G-protein coupled

August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends Although studies have focused on the G-protein signaling state, the mechanism for β-arrestin signaling

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Cell surface expression was severely reduced to ≤18% of wild-type (WT) for 11, modestly reduced to 66% 11 with severely reduced cell surface expression, restoration to ≥57% of WT levels was achieved for 6 by treatment with 1 µM CAN1404 for 24 h, and a corresponding increase in FSH-induced signaling was observed

Prostaglandin (PG) signaling regulates a wide variety of physiological and pathological processes, including Many G-protein-coupled receptors (GPCRs) including EP4 are localized in cilia for modulating cAMP signaling During development, PGE2 signaling regulates embryogenesis, hepatocyte differentiation, hematopoiesis This review outlines recent advances in understanding the functions and mechanisms of prostaglandin signaling

., stimulatory or blocking effects on different downstream signaling pathways). This emphasizes the importance of the Gi/o (pertussis toxin-sensitive G proteins, whose βγ subunits activate multiple signals, including ERK1/2) in regulating parathyroid hormone secretion. (f) the presence of CaSR autoantibodies that operated as biased allosteric modulators of CaSR, and (g) Our observations with these prominent commonalities may provide new insights into the phenotype and characteristics

These receptors initiate intracellular signaling cascades upon activation, ultimately regulating a myriad (cAMP), calcium mobilization, and extracellular signal-regulated kinase (ERK) activation [1]. assay [6], mini-G recruitment assay [7], GRK and β-arrestin recruitment assays [8]), G protein activation Gilman, A.G., G proteins: transducers of receptor-generated signals.  Nature, 2020. 577(7790): p. 432-436. 6.     

Protein Interaction "The calcium-sensing receptor is a homodimeric class C G protein-coupled receptor protein-dependent signaling via twin Cysteine-rich domains linked to transmembrane heptahelical (HH) It plays a key role in the regulation of human calcium and thus mineral metabolism. In contrast, a single WT HH bundle was insufficient for maximal signaling and there was no functional not via combined in-trans and in-cis signaling.

encode a variety of bioactive small molecules with growing evidence for N-acyl amides as being important signaling meningitidis and identified 30 N-acyl amides with representative members serving as agonists of the G-protein Both groups of metabolites suppress anti-inflammatory interleukin-10 signaling in human macrophage cell

GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and The molecular diversity of GPCR signaling systems is likely to be closely associated with disease-associated of protein expression patterns, cellular stress responses and DNA integrity management. understanding of this function of GPCRs is likely to significantly augment our ability to further employ these proteins

October 2022 "Numerous physiological processes in insects are tightly regulated by neuropeptides and Although they form an ancient signaling system, there is still a great deal of variety in neuropeptides Here, 33 neuropeptide precursors and 48 putative neuropeptide G protein-coupled receptor (GPCR) genes Additionally, we discovered that the neuropeptide signaling systems of Sternorrhyncha were very different groundwork for the creation of novel D. vitifoliae management strategies that specifically target these signaling

conformational consequences of the differential activity of cannabidiol with two endocannabinoid-activated G-protein-coupled to modulate different receptors in the endocannabinoid system, some of which belong to the family of G-protein-coupled investigate the interacting determinants of CBD in two closely related endocannabinoid-activated GPCRs, the G-protein-coupled

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular Different agonists can promote differential receptor-induced signaling responses - termed bias - potentially Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements

September 2022 "Receptor-activity-modifying proteins (RAMPs) are ubiquitously expressed membrane proteins that associate with different G protein–coupled receptors (GPCRs), including the parathyroid hormone However, it is unknown whether and how RAMP proteins may affect PTH1R function. Using different optical biosensors to measure the activation of PTH1R and its downstream signaling, we the PTH-mediated Gi3 signaling sensitivity.

Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets

Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated However, GRKs have not been directly implicated in regulation of the amyloid-β (Aβ) pathogenic cascade recruitment of the scaffolding protein β-arrestin 2 (βarr2) to APH1A and γ-secretase-mediated Aβ generation the βarr2 finger loop domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin complex, which regulates insight into the molecular and structural determinants of the APH1A-βarr2 interaction that critically regulate