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a single drug, peroxisome proliferator-activated receptor (PPAR) α/γ agonist saroglitazar, has been approved

into how EBI2 is activated by an oxysterol ligand and will facilitate the development of therapeutic approaches

Applied to HIV-1 envelope glycoproteins gp120, our quantitative analysis revealed agonist-like properties

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

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

These advances have paved the way for development of novel ligands for different therapeutic applications

Besides their appearance on the (illicit) drug market, e.g. as new psychoactive substances, their potential therapeutic application is increasingly explored.

effects, and tools to explore the ORs nature and function, various (poly)pharmacological ligand design approaches

Methods Proliferation, migration and apoptosis assays were performed in ovarian cancer cells after fentanyl Immunoblotting approach was used to analyze signaling involved in fentanyl’s action focusing on EGFR.

In vitro, SACC cell proliferation and apoptosis were evaluated using Cell Counting Kit-8 and colon formation

September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the FDA-approved

The functional relevance of C5aR2 appears to be context-dependent compared to the C5aR1, which has received

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

The PVT appears to provide stimulus salience encoding in a dose- and NPS-dependent manner.

the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked by the application

Cell cycle and apoptosis were determined by flow cytometry.

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

Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach

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

and voltage-dependent current caused by MRGPRB2 activation were blocked by U73122 (PLC blocker) or 2-APB

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.

Alterations in gene expression appear in pathways related to primary cilia (PC).

results, we investigated the role of the CBD compound on the CB1 receptor using similar computational approaches

We have previously shown, using a combination of experimental and simulation approaches, that membrane

We demonstrate with the application of ML methods that it is possible to identify the key interactions This approach can be readily applied to any drug target."

Subacute SCI is mainly characterized by neuronal apoptosis, axonal demyelination, Wallerian degeneration

between 5-HT2A and TrkB in vitro and in vivo using co-immunoprecipitation and biophysical and biochemical approaches

protein-coupled receptors, such as the prokineticin receptors, and regulates energy expenditure and appetite

breast cancer "Quantitative systems pharmacology (QSP) modeling is an emerging mechanistic computational approach , the modularized QSP platform can be readily reproduced, expanded for new species of interest, and applied

receptor CXCR4 coupled with site-directed mutagenesis and bioluminescence resonance energy transfer approaches