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October 2022 "Study of small molecule binding to live cells provides important information on the characterization of ligands pharmacologically. Here we developed and validated a label-free, liquid chromatography-mass spectrometry (LC-MS) based cell Competition binding analysis by titration of five known ligands suggested a good correlation with their This versatile method allows quantitative characterization of ligand binding to cell surface expressed

October 2022 "Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled

unveiled a new antifibrotic cGAS/STING signaling pathway that suppresses pathological angiogenesis in liver We showed that cGAS expression was induced in fibrotic liver and kidney, but suppressed in endothelial cells. cGAS genetic deletion promoted liver and kidney fibrosis and pathological angiogenesis, including receptor (GPCR)-based antagonist that blocks the profibrotic activity of endothelial YAP, attenuated liver Further, pharmacological targeting of cGAS/STING-YAP axis exhibits the potential to alleviate liver and

Neural PKA signaling is regulated by afferent and peripheral efferent signals that link specific neural cell populations to the regulation of metabolic processes in adipose tissue, liver, pancreas, adrenal While limited, human studies infer differential regulation of the PKA system in obese compared to lean

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein However, Gpr3-deficient mice display several adverse phenotypes, including elevated anxiety-like behavior by robust microglial and astrocytic hypertrophy, which suggest a protective glial response that may limit

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A diverse pharmacopeia of cannabinoid ligands is available, which has led to considerable advancements However, until recently, most CB2 ligands were highly lipophilic and as such, not optimal for clinical A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties We review the current state of CB2 ligand development and progress in optimizing physicochemical properties

A special emphasis is placed on knowledge gaps, challenges, and limitations to evaluate the underpinnings

many aspects including the assembly of the extracellular and transmembrane domains, the shape of the ligand-binding

In this review, we provide an accessible summary of the literature on Alzheimer's disease and the therapeutic

activated by these G protein-coupled receptors based on several factors, including the nature of the ligand These effects include reducing the atherosclerotic plaque area, improving the serum lipid profile, attenuation encouraging results, testing CXCR1/2 inhibitors in clinical trials could be of a great importance to limit

Current literature strongly establishes increased levels and activity of GRK2 in multiple models of CVD

conformational basis for signaling bias, which would have enabled the rational design of biased GRCR ligands

This compound has vastly reduced brain penetration and is devoid of significant off-target liability.

We also present a detailed protocol for monitoring cAMP levels in live cells expressing endogenous or

NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in Cell Membranes and Living receptor (H3R) biosensor that allowed the detection of both (partial) agonism and inverse agonism on living cells in a microplate reader assay format upon stimulation with H3R ligands. injections in time and evaluating its compatibility with photopharmacological ligands that contain a light-sensitive azobenzene moiety for photo-switching.

"Genetically encoded fluorescent biosensors allow intracellular signaling dynamics to be tracked in live

GPR3 is unique in its ability to constitutively activate the Gαs protein without a ligand, which elevates

Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, little Synaptamide suppressed osteoclastogenesis induced by receptor activator of nuclear factor-kappa B ligand Our study suggested that ligands of GPR110, such as synaptamide, might be a useful drug for osteoporotic

August 2022 "Aims: The pathophysiological mechanism(s) underlying non-alcoholic fatty liver disease (

motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural ligand Evidence demonstrated that the ligation of SDF-1 to CXCR4 initiates several intracellular signaling pathways

detected by the Boyden chamber migration assay, performed on macrophages derived from both the THP-1 cell line

In the presence of its ligand, we show significant upregulation of H2R nuclear translocation kinetics In this aspect, our present data shed new light on the unexplored H2R signaling mechanisms.

These structures reveal an agonist binding site for the oxysterol and a potential ligand entrance site exposed to the lipid bilayer. Together, these findings provide new insight into how EBI2 is activated by an oxysterol ligand and will facilitate the development of therapeutic approaches that target EBI2-linked diseases."

The fusion strategies explored here are likely applicable to cryo-EM interrogation of other GPCRs and

During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent

August 2022 "The X-linked form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism

highly conserved NPXXY motif can be subject to different conformational changes in response to biased ligands

changed conformation of the receptor and consequently activated signaling pathways, and also may shed light

A major pan-receptor focus has been to identify GPCR-selective ligands that have bias in G protein-dependent this field has exploded during the past two decades, it is only recently that highly β-arrestin biased ligands