Search Results
355 items found for "Ya-Tzu Li"
- Dr. GPCR Virtual Cafe with Matthew Eddy - New date!
Don't miss the chance to listen to his latest research on the field.
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopeia: past, present, and future
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
- Molecular targets of psychedelic-induced plasticity
A special emphasis is placed on knowledge gaps, challenges, and limitations to evaluate the underpinnings
- AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors
many aspects including the assembly of the extracellular and transmembrane domains, the shape of the ligand-binding
- Adenosine receptor signalling in Alzheimer's disease
In this review, we provide an accessible summary of the literature on Alzheimer's disease and the therapeutic
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
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
- GRK2 in cardiovascular disease and its potential as a therapeutic target
Current literature strongly establishes increased levels and activity of GRK2 in multiple models of CVD
- Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling
conformational basis for signaling bias, which would have enabled the rational design of biased GRCR ligands
- Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin recept
This compound has vastly reduced brain penetration and is devoid of significant off-target liability.
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
We also present a detailed protocol for monitoring cAMP levels in live cells expressing endogenous or
- A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in...
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.
- In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors
"Genetically encoded fluorescent biosensors allow intracellular signaling dynamics to be tracked in live
- 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
- 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, 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
- RGS7-ATF3-Tip60 Complex Promotes Hepatic Steatosis and Fibrosis by Directly Inducing TNFα
August 2022 "Aims: The pathophysiological mechanism(s) underlying non-alcoholic fatty liver disease (
- MSX-122: Is an effective small molecule CXCR4 antagonist in cancer therapy?
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
- G protein-coupled receptor 21 in macrophages: An in vitro study
detected by the Boyden chamber migration assay, performed on macrophages derived from both the THP-1 cell line
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
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.
- Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response
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."
- Fusion protein strategies for cryo-EM study of G protein-coupled receptors
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
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
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
August 2022 "The X-linked form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism
- The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor
highly conserved NPXXY motif can be subject to different conformational changes in response to biased ligands
- Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic di
changed conformation of the receptor and consequently activated signaling pathways, and also may shed light
- Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior...
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
- 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
- 📅 Dr. GPCR Summit 2022 is less than a month away!
Come live and breathe GPCRs with us and don’t forget to submit your abstract.
- Episode 86 of the Dr. GPCR podcast with Dr. Nicole (Nicki) Perry-Hauser is now available!
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