Search Results
521 items found for "Jespers W"
- GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates axonal...
GPR3 is unique in its ability to constitutively activate the Gαs protein without a ligand, which elevates Herein, we investigated retinal GPR3 expression and its possible involvement in axonal regeneration after Surprisingly, RGCs in GPR3 knockout mice were vulnerable to neural death during aging without affecting In addition, regenerating axons were further stimulated when GPR3 was upregulated in RGCs, and the effect was further augmented when combined with zymosan treatment.
- Aβ peptides stabilize GPCRs in inactive form and trigger inverse agonism in Alzheimer's disease
August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), which
- The integrin ligand SVEP1 regulates GPCR-mediated vasoconstriction via integrins α9β1 and α4β1
Genetic variants in ITGA9, which encodes the α9 subunit of integrin α9β1, and SVEP1, a ligand for integrin We determined whether SVEP1 and integrin α9β1 can regulate VSMC contraction."
- G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions...
GRK2/β-arrestin2 play multiple roles in the pathological mechanisms of a wide range of diseases including
- GPR110, a receptor for synaptamide, expressed in osteoclasts negatively regulates osteoclastogenesis
Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, In this study, we found, for the first time, that the expression of GPR110 increased during osteoclastogenesis Considering that synaptamide is the endogenous metabolite of DHA, we hypothesized that DHA may inhibit
- RGS7-ATF3-Tip60 Complex Promotes Hepatic Steatosis and Fibrosis by Directly Inducing TNFα
Here, we sought to investigate the role of Regulator of G Protein Signaling 7 (RGS7) in hyperlipidemia-dependent
- TAS2R supports odontoblastic differentiation of human dental pulp stem cells in the inflammatory...
In this study, we aimed to explore the role of TAS2R in odontoblastic differentiation of hDPSCs in the inflammatory and healthy pulp tissues from the patients. hDPSCs isolated from the healthy pulp tissues were The expression markers related to odontoblastic differentiation of hDPSCs were observed by qPCR and chemical The G protein and intracellular Ca2+ were detected, respectively, by qPCR and Fluo-4AM Ca2+ fluorescent
- MSX-122: Is an effective small molecule CXCR4 antagonist in cancer therapy?
cytokines along with their receptors, are involved in various biologic processes and regulation of a wide pathways, regulating cell proliferation, survival, chemotaxis, migration, angiogenesis, adhesion, as well
- A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in...
Uterine Corpus Endometrial Carcinoma (UCEC) isa malignanttumorofendometrium epithelial, whichis alsooneofthemostcommonfemalereproductivesystemtumors
- G protein-coupled receptor 21 in macrophages: An in vitro study
THP-1 cells were activated and differentiated into either M1 or M2 macrophages.
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell and tissue types. In this study, for the first time, we demonstrate the nuclear localization of H2R in lymphatic endothelial In the presence of its ligand, we show significant upregulation of H2R nuclear translocation kinetics Using fluorescently tagged histamine, we explored H2R-histamine binding interaction, which exhibits a
- Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response
Here, we report the cryo-EM structures of an EBI2-Gi signaling complex with its endogenous agonist 7α Mutations within the oxysterol binding site and the Gαi interface attenuate G protein signaling and abolish
- Helix 8 in chemotactic receptors of the complement system
Here, we discuss recent crystal structures of inactive C5aR1 in terms of an inverted orientation of helix By comparing two C5aR receptors C5aR1 and C5aR2 we explained differences between their signaling pathways By means of molecular dynamics we explained why C5aR2 cannot transduce signal through the G protein pathway
- Tracking receptor motions at the plasma membrane reveals distinct effects of ligands on CCR5...
Here, we investigated this issue in living cells for the CC chemokine receptor 5 (CCR5), a major receptor We used TIRF microscopy and a statistical method to track and classify the motion of different receptor We showed a diversity of ligand-free forms of CCR5 at the cell surface constituted of various oligomeric These forms were stabilized differently by distinct ligands. stimulation restricted the mobility of CCR5 and led to its clustering, a feature depending on β-arrestin, while
- Structures of β 1-adrenergic receptor in complex with Gs and ligands of different efficacies
Here, we investigate how a GPCR activates G-proteins upon binding ligands with different efficacies. We report the cryo-EM structures of β1-adrenergic receptor (β1-AR) in complex with Gs (GαsGβ1Gγ2) and a partial agonist or a very weak partial agonist, and compare them to the β1-AR-Gs structure in complex uncover that the intermediate state complex comprising β1-AR and nucleotide-free Gs is more stable when
- Fusion protein strategies for cryo-EM study of G protein-coupled receptors
However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack similar strategy has the potential to broadly facilitate cryo-EM structure determination of GPCRs alone without Here, we address this shortcoming by exploring different fusion protein designs, which lead to structures
- Novel interaction between neurotrophic factor-α1/carboxypeptidase E and serotonin receptor, 5-HTR1E,
We uncovered a novel neuroprotective mechanism involving interaction between neurotrophic factor-α1 ( Treatment of 5-HTR1E stable cells with NF-α1/CPE increased pERK 1/2 and pCREB levels which prevented
- GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting
family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination, GRK2, which The medium chain fatty acid receptor GPR84 as well as formyl peptide receptor 2 (FPR2), receptors expressed In this study, we investigated the effects of GRK2 inhibitors on neutrophil functions induced by GPR84
- Multifunctional role of GPCR signaling in epithelial tube formation
Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin We also report on unexpected Fog-independent roles for Smog in maintaining epithelial integrity and organizing Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent
- GPCR kinases generate an APH1A phosphorylation barcode to regulate amyloid-β generation
Here, we determine that GRKs phosphorylate a non-canonical substrate, anterior pharynx-defective 1A ( Significantly, we show that GRKs generate distinct phosphorylation barcodes in intracellular loop 2 ( ICL2) and the C terminus of APH1A, which differentially regulate recruitment of the scaffolding protein between the βarr2 finger loop domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin complex, which
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
We have previously shown interaction between PKR2 and anosmin 1 in vitro. In the current report we present evidence of the modulation of PK2/PKR2 activity by anosmin 1, since We also show that the N-terminal region of anosmin 1, capable of binding to the PK2-binding domain of The whey acidic protein domain (WAP) is necessary for this modulatory activity, although data from GST type III domain 1 (FnIII.1) suggest the cysteine-rich (CR) and the FnIII.1 domains could assist the WAP
- Molecular basis for ligand modulation of the cannabinoid CB 1 receptor
CB1 receptor is the most abundant G protein coupled receptor (GPCR) in the central nervous system, which These advances have paved the way for development of novel ligands for different therapeutic applications 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.
- The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor
focused on the G-protein signaling state, the mechanism for β-arrestin signaling by CB1 is not yet well
- Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic di
In this study, R68W and V162A were analyzed to whether they show a bias to Gαs or Gαq/11 proteins. Their functionality in terms of cAMP production via Gαs protein coupling was decreased compared to the wild-type R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type receptor.
- Production of human A2AAR in lipid nanodiscs for 19F-NMR and single-molecule fluorescence...
Production of human A 2A AR in lipid nanodiscs for 19 F-NMR and single-molecule fluorescence spectroscopy "We We explain in detail steps shared between the two sample preparation strategies, including expression For complete details on the use and execution of this protocol, please refer to Wei et al. (2022) and
- Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior...
two decades, it is only recently that highly β-arrestin biased ligands for the dopamine D1 receptor were We now summarize important pharmacological, molecular, and cellular studies relevant to D1-mediated β-arrestin-related We discuss the importance of understanding the translatability of cell and animal models to have more
- In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
Additionally, several variables are discussed that one should consider when attempting to compare functional
- Episode 87 of Dr. GPCR Podcast is available now!
Listen to her talk about her work and her transition to PI in Belfast. Watch the full video with a paid @DrGPCR Ecosystem membership or listen wherever you get your podcast