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158 items found for "Can Cao"
- Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery
Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors (GPCRs) can form biologically active homodimers or heterodimers which drive specific signaling pathways that can But how can we target GPCR dimers? Recent studies found that peptides derived from the transmembrane region of GPCRs can block the formation
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
excitatory neurotransmitter of the nervous central system, L-glutamate, and mGlu5 receptor activity can illustrate how access to high-resolution structures of GPCRs in complex with allosteric modulators can
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- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
Showing that this spatially biased signaling through arrestins can influence transcriptional responses addition to endosomal signaling, GPCRs are also known to localize to the Golgi apparatus, where they can Activation of nuclear GPCRs, such as the metabotropic glutamate receptor 5 (mGluR5), can lead to sustained both temporal and spatial components, sustained signaling responses from intracellular compartments can Additionally, the conditions within endosomes, such as low pH and high protease activity, can degrade
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs
- Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells...
These data indicate that sea bass GnIHR signals can be transduced through the PKA and PKC pathways, and GnIH can interfere with kisspeptin actions by reducing its signaling.
- Enhanced membrane binding of oncogenic G protein αqQ209L confers resistance to inhibitor YM-254890
They can also function independently of GPCR activation upon acquiring mutations that prevent GTPase YM-254890 (YM) can inhibit signaling by both GPCR-activated wild type αq and GPCR-independent αqQ209L
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- Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and ...
and Heterodimer Information flow from a source to a receiver becomes informative when the recipient can that GPCRs may physically interact with each other has led to the hypothesis that their dimeric state can
- The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor
Studies have indicated that transmembrane helix 7 (TMH7) and the highly conserved NPXXY motif can be
- 📰 GPCR Weekly News, March 6 to 12, 2023
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- Residency time of agonists does not affect the stability of GPCR-arrestin complexes
Here, we ask the question whether agonists with very slow off-rates can cause the formation of particularly
- The integrin ligand SVEP1 regulates GPCR-mediated vasoconstriction via integrins α9β1 and α4β1
We determined whether SVEP1 and integrin α9β1 can regulate VSMC contraction."
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- In Vitro and In Silico Characterization of Kurarinone as a Dopamine D 1A Receptor Antagonist and ...
Since studies have indicated that flavonoids can target brain GPCRs and provide neuroprotection via inhibition appreciable D2LR and D4R agonism and D1R antagonism, kurarinone might be a potential compound that can
- Dynamic GPCR activation revealed through time-resolved Cryo-EM
With this high-resolution, dynamic view of GPCR activation, scientists can better tackle diseases by Beyond GPCRs, the methods and insights from this study can be applied to other fast, transient biological
- Therapeutic validation of an orphan G protein‐coupled receptor
., 2011), although it is widely accepted that medium‐chain fatty acids (MCFAs) can bind to and activate and 2. which ligands can be used as tool compounds to study the function and biology of this receptor distinct functional outcomes of agonist ligands (Pillaiyar et al., 2018) with biased properties which can
- Platelets in the NETworks interweaving inflammation and thrombosis
In particular, platelets can activate neutrophils to form neutrophil extracellular traps (NETs). Furthermore, NETs can be found in the lung and other tissues and are associated with an increased mortality
- Molecular insights into psychedelic drug action
knowledge regarding the molecular details of psychedelic drug actions and suggest that these discoveries can
- Rescue of Cell Surface Expression and Signaling of Mutant Follicle-Stimulating Hormone Receptors
Here we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone Therefore, CAN1404 acts as a pharmacological chaperone and can rescue cell surface expression and function
- Research Network on Signal Transduction (ERNEST) has established an Emergency Fund for Ukrainian ...
scientific mission grants to Ukrainian researchers who have been recently displaced by the war, or those who can
- Emerging approaches for decoding neuropeptide transmission
These complex properties have driven the need for development of specialized tools that can sense neuropeptide
- Glyco-sulfo hotspots in the chemokine receptor system
Schjoldager KT et al. 2020), and usually capped by a single sialic acid, although, in rare cases glycans can This effect could be driven by a specific carrier or it can potentially be related with the increase sulfation are important PTMs in chemokine receptor biology and pharmacology however the reported effects can Moreover, sulfated mCCR2 peptides can outcompete available chemokines, decreasing retinal degradation
- Posttranslational modifications in GPCR internalization
However, many studies over the past decade have reported that internalized membrane receptors can trigger
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- The expression and clinical significance of GPR39 in colon cancer
GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival.
- 📰 GPCR Weekly News, March 18 to 24, 2024
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