Search Results
264 items found for "IJzerman AP"
- GRK2 in cardiovascular disease and its potential as a therapeutic target
Currently-approved treatments have improved patient outcomes, but therapies to stop or reverse HF are
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
They have participated in various cellular processes such as cell proliferation, migration, apoptosis
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
molecular tools to study G protein-coupled receptors (GPCRs) and can be used for a range of different applications Further, we show that 14 can be used as a tool for fragment-based screening approaches.
- Exploring pharmacological inhibition of G q/11 as an analgesic strategy
Experimental approach: We used a series of behavioural assays to evaluate the acute responses of mice
- In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors
the principle of Förster resonance energy transfer (FRET), and we have recently developed a simple approach Our approach, described in detail here, uses adeno-associated viruses infused intracerebrally in order Hence, it has wide applicability across a spectrum of neuroscience research, ranging from the study of
- RGS7-ATF3-Tip60 Complex Promotes Hepatic Steatosis and Fibrosis by Directly Inducing TNFα
a single drug, peroxisome proliferator-activated receptor (PPAR) α/γ agonist saroglitazar, has been approved
- Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response
into how EBI2 is activated by an oxysterol ligand and will facilitate the development of therapeutic approaches
- Tracking receptor motions at the plasma membrane reveals distinct effects of ligands on CCR5...
Applied to HIV-1 envelope glycoproteins gp120, our quantitative analysis revealed agonist-like properties
- 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 structure determination of GPCRs alone without signaling protein, the critical determinants that make this approach The fusion strategies explored here are likely applicable to cryo-EM interrogation of other GPCRs and
- Multifunctional role of GPCR signaling in epithelial tube formation
gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog) activates Rho1 signaling to drive apical regulate Rho kinase accumulation and myosin activation in the medioapical region of cells to control apical
- Molecular basis for ligand modulation of the cannabinoid CB 1 receptor
These advances have paved the way for development of novel ligands for different therapeutic applications
- In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
Besides their appearance on the (illicit) drug market, e.g. as new psychoactive substances, their potential therapeutic application is increasingly explored.
- Opioid Ligands Addressing Unconventional Binding Sites and More Than One Opioid Receptor Subtype
effects, and tools to explore the ORs nature and function, various (poly)pharmacological ligand design approaches
- CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma via...
In vitro , SACC cell proliferation and apoptosis were evaluated using Cell Counting Kit-8 and colon formation
- Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid...
Methods Proliferation, migration and apoptosis assays were performed in ovarian cancer cells after Immunoblotting approach was used to analyze signaling involved in fentanyl’s action focusing on EGFR.
- Multifunctional role of GPCR signaling in epithelial tube formation
gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog) activates Rho1 signaling to drive apical regulate Rho kinase accumulation and myosin activation in the medioapical region of cells to control apical
- Neuropeptide S Encodes Stimulus Salience in the Paraventricular Thalamus
The PVT appears to provide stimulus salience encoding in a dose- and NPS-dependent manner.
- Delineation of GPR15 receptor-mediated Gα protein signaling profile in recombinant mammalian cell
the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked by the application
- GRK3 is a poor prognosticator and serves as a therapeutic target in advanced gastric adenocarcinoma
2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the FDA-approved
- C5aR2 receptor: The genomic twin of the flamboyant C5aR1
The functional relevance of C5aR2 appears to be context-dependent compared to the C5aR1, which has received
- Lipid Modulation of a Class B GPCR: Elucidating the Modulatory Role of PI(4,5)P 2 Lipids
In this work, we applied MD simulations supported by native mass spectrometry (nMS) to study lipid interactions Interestingly, we find that in contrast to class A GPCRs, PI(4,5)P2 appear to stabilize the inactive
- Ligands can differentially and temporally modulate GPCR interaction with 14-3-3 isoforms
Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach
- Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5...
Here, we used a proximity ligation assay (PLA)–based approach for the in situ visualization and quantification Using the PLA approach combined with epitope tagging, we detected homo-dimers of human SST2 in GH3, A7
- Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...
In contrast, blocking AVPR2 with a selective FDA-approved antagonist, tolvaptan, reduced cell growth. Combinatorial use of AVPR1A and AVPR2 antagonists promoted apoptosis synergistically in CRPC cells.
- Interacting binding insights and conformational consequences of the differential activity of...
results, we investigated the role of the CBD compound on the CB1 receptor using similar computational approaches
- Primary cilia and SHH signaling impairments in human and mouse models of Parkinson’s disease
Alterations in gene expression appear in pathways related to primary cilia (PC).
- A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Hypoxia: New..
Cell cycle and apoptosis were determined by flow cytometry.
- PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal...
and voltage-dependent current caused by MRGPRB2 activation were blocked by U73122 (PLC blocker) or 2-APB