Search Results
Results found for "Helen Su"
- Dr. GPCR Virtual Cafe with Matthew Eddy - New date!
It's a great opportunity to get warmed up for the upcoming Summit starting the next Monday.
- Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system, emerging...
selectively targeting CB2 receptors with respect to schizophrenia, the studies discussed below could suggest
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopeia: past, present, and future
Promising preclinical data support the applicability of CB2 activation in autoimmune and inflammatory
- TRPM3 in the eye and in the nervous system - from new findings to novel mechanisms
calcium-permeable cation channel TRPM3 can be activated by heat and the endogenous steroid pregnenolone sulfate
- Molecular insights into psychedelic drug action
Here we review the current knowledge regarding the molecular details of psychedelic drug actions and suggest
- Adenosine receptor signalling in Alzheimer's disease
Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets In this review, we provide an accessible summary of the literature on Alzheimer's disease and the therapeutic strategies, including allosterism and the targeting of oligomers, which may increase drug discovery success
- GRK2 in cardiovascular disease and its potential as a therapeutic target
These data support the premise that GRK2 should be at the forefront of a novel investigative drug search GPCRs, describes the structure and functions of GRK2 in cardiac function and maladaptive pathology, and summarizes
- Posttranslational modifications in GPCR internalization
Here, this review summarizes different PTMs in GPCR internalization and analyzes their significance in
- Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling
Our analysis suggests that the structures of GPCRs bound to these interaction partners available today there are no generalizable GPCR conformations conducive to binding a particular type of partner; (ii) subtle
- Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin recept
In summary, a potent and selective APJ agonist suitable for in vivo studies of APJ in peripheral tissues
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
tetramethylrhodamine (TAMRA)-labeled CCR2 ligands were designed, synthesized, and tested for their suitability
- Exploring pharmacological inhibition of G q/11 as an analgesic strategy
showed that activation of Gq/11 proteins by G-protein coupled receptors has pro-nociceptive properties, suggesting
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
application to cell-based kinetic studies "G protein-coupled receptors (GPCRs) are an important receptor superfamily As well, the GloSensor-22F biosensor had a superior signal-to-background ratio and the effect of temperature
- Aβ peptides stabilize GPCRs in inactive form and trigger inverse agonism in Alzheimer's disease
This paradox solicits urgent attention to find a suitable justification for disturbed neurotransmission
- The integrin ligand SVEP1 regulates GPCR-mediated vasoconstriction via integrins α9β1 and α4β1
Genetic variants in ITGA9, which encodes the α9 subunit of integrin α9β1, and SVEP1, a ligand for integrin
- G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions...
This review summarizes the roles of GRK2/β-arrestin2 in immune cell function and focuses on the pathological
- GPR110, a receptor for synaptamide, expressed in osteoclasts negatively regulates osteoclastogenesis
Synaptamide suppressed osteoclastogenesis induced by receptor activator of nuclear factor-kappa B ligand But GPR110 knockout and subsequent rescue experiments revealed a pivotal role of GPR110 in the attenuation These results suggest that synaptamide/GPR110 signaling negatively regulates osteoclastogenesis. Our study suggested that ligands of GPR110, such as synaptamide, might be a useful drug for osteoporotic
- MSX-122: Is an effective small molecule CXCR4 antagonist in cancer therapy?
August 2022 "Chemokines, a subgroup of cytokines along with their receptors, are involved in various of SDF-1 to CXCR4 initiates several intracellular signaling pathways, regulating cell proliferation, survival
- G protein-coupled receptor 21 in macrophages: An in vitro study
August 2022 "GPR21 is an orphan and constitutively active receptor belonging to the superfamily of G-Protein
- A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in...
protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
August 2022 "Histamine exerts its physiological functions through its four receptor subtypes. In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled
- Helix 8 in chemotactic receptors of the complement system
An analysis of mutual interactions of subunits in the C5aR1-G protein complex has provided new insights details of local and global changes in the transmembrane domain induced by interactions with the Gα subunit
- Tracking receptor motions at the plasma membrane reveals distinct effects of ligands on CCR5...
August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational used TIRF microscopy and a statistical method to track and classify the motion of different receptor subpopulations We showed a diversity of ligand-free forms of CCR5 at the cell surface constituted of various oligomeric These results suggest a link between receptor activation and immobilization.
- Structures of β 1-adrenergic receptor in complex with Gs and ligands of different efficacies
Molecular dynamics simulations support the local conformational flexibilities and different stabilities
- Fusion protein strategies for cryo-EM study of G protein-coupled receptors
GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly successful determination of GPCRs alone without signaling protein, the critical determinants that make this approach successful
- Novel interaction between neurotrophic factor-α1/carboxypeptidase E and serotonin receptor, 5-HTR1E,
HTR1E stable cells with NF-α1/CPE increased pERK 1/2 and pCREB levels which prevented a decrease in pro-survival Cell survival assay in β-arrestin Knockout HEK293 cells showed that the NF-α1/CPE-5-HTR1E-mediated protection Immunofluorescence studies showed 5-HTR1E and NF-α1/CPE are highly expressed and co-localized on cell surface
- GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting
GRK2 was shown to be expressed in human neutrophils and analysis of subcellular fractions revealed a
- GPCR kinases generate an APH1A phosphorylation barcode to regulate amyloid-β generation
August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated Here, we determine that GRKs phosphorylate a non-canonical substrate, anterior pharynx-defective 1A (
- Multifunctional role of GPCR signaling in epithelial tube formation
Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. 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
glutathione-S-transferase) and analysis of the N267K mutation in the fibronectin type III domain 1 (FnIII.1) suggest Our data support the idea of a modulatory role of anosmin 1 in the biological effects controlled by the

