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55 items found for "Lina Yang"
- Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking: ...
Modes "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes that regulate a wide range
- Targeted Therapies to Reduce Side Effects in Modern Drug Development
Modern drug development approaches include a range of techniques leveraging structural biology, immunology
- Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR...
fluorescent GPCR ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with semi-quantitative receptor mapping in living cells and validated the specific expression of A2BAR in CRC cell lines
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
fragment- and seven lead-like compounds were confirmed to bind to the allosteric site with affinities ranging
- Successful prednisolone or calcimimetic treatment of acquired hypocalciuric hypercalcemia caused...
diseases, (d) showed spontaneously fluctuating Ca levels from approximately normal to near fatally high ranges
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
fragment- and seven lead-like compounds were confirmed to bind to the allosteric site with affinities ranging
- Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Interface
We show that besides classical hydrogen bonds, weak polar interactions such as O-HC, O-Br, and long-range
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs
- A Model for the Signal Initiation Complex Between Arrestin-3 and the Src Family Kinase Fgr
Arrestins regulate a wide range of signaling events, most notably when bound to active G protein-coupled
- The development of modulators for lysophosphatidic acid receptors: A comprehensive review
Lysophosphatidic acids (LPAs) are bioactive phospholipids implicated in a wide range of cellular activities
- GPCRs are not simple on-off switches: deep dive into GPCR-ligand interactions
GPCRs are present in a range of conformations, and the binding of a ligand, as well as interactions with desensitization), the same drug acting on the same receptor in the same cellular context can produce a range different ligands inducing unique GPCR conformations that selectively activate specific cellular outcomes linked
- GPCRS: AN ODYSSEY FROM STRUCTURE, SIGNALING AND REGULATION TO THERAPEUTICS
Coupled with their ability to respond to a highly diverse range of chemical stimuli, they represent the
- Chemical signaling regulates axon regeneration via the GPCR-Gqα pathway in Caenorhabditis elegans
Chemical communication controls a wide range of behaviors via conserved signaling networks.
- Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled ..
Several members of MRGPRs are also expressed in mast cells, macrophages, and in cardiovascular tissue, linking Consequently, the dynamic range for IL-6 detection as an assay for β-alanine-mediated activation of MRGPRD
- Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the ...
Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the range of
- Unveiling GPCR Priming: The Hidden Synergy in Cellular Signalling
could unveil new dimensions of GPCR functionality and offer innovative approaches to treating a wide range
- Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
to predict subtype-selective ligands for dopamine receptors and adenosine receptors (He, Ben, Kuang, Wang & Kong, 2016; Kuang, Feng, Hu, Wang, He & Kong, 2016). 5.
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
However, the receptors that these medicines target have been described as the ‘low-hanging’ fruit, and While these small protein GPCRs are valuable drug targets linked to serious diseases, many remain undrugged There are approximately 800 human GPCRs in the superfamily, controlling a broad range of physiological The remaining non-sensory receptors, with functions more readily linked to pathology, are currently the Figure 5: In an in vitro functional signaling assay on a human monocytic cell line, OB-004 demonstrated
- From DNA day to GPCR genomics
The completion of the Human Genome Project revealed that GPCR genes in the human genome range from approximately
- VAMP2: a crucial player in the delivery of MOR to the synapse
You can consult the article at the following link: https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function Wang, F., X. Chen, X. Zhang, and L. Ma. 2008.
- Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery
“ A substitution of one amino acid by another in a protein can have effects ranging from negligible to can provide a comprehensive understanding of how drugs interact with different receptor regions and link
- 🤯Mind-blowing GPCR Scoops! Discover the Latest Breakthroughs! ⦿ Nov 18 - 24, 2024
High-affinity agonists reveal recognition motifs for the MRGPRD GPCR Chunyu Wang , Yongfeng Liu , Marion Direct line to the Dr.
- Unlocking Cell's Secrets: Spontaneous β-Arrestin-Membrane Preassociation Drives Receptor-Activation
., Wang, J.K., Bauer, B., Townshend, R.J.L., Hollingsworth, S.A., Olivieri, J.E., Xu, H.E., Sommer, M.E
- Overview of adhesion GPCRs self-activation
., Wang, N., Xu, Z., Xia, R., Liang, J., Duan, Y., Yin, H., Xiong, Y., Zhang, A., Guo, C., Chen, Z.,
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
receptor internalization, with the same observations made for CCR2-expressing THP-1 monocytic cell line In line, β-Arrestin KO cells showed a major reduction in CCL14 scavenging by CCR1, in contrast with a Wang et al. 2009; R. J.
- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
The clinical relevance of understanding these signaling mechanism is linked with the fact that dysregulation For instance, aberrant endosomal signaling by GPCRs has been linked to disorders such as cancer, neurodegenerative N., Castro, M., Wang, B., Bouley, R., Potts, J. T., Gardella, T. J., & Vilardaga, J. P. (2009).
- Structural landscape of the Chemokine Receptor system
N-terminus to the extracellular tip of the seventh transmembrane helix (TM7) near ECL3, while the other links activation will pave the way for significant advancements in the development of therapeutics for a wide range