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376 items found for "Helen Su"
- Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes
type and receptor activation state G protein-coupled receptors (GPCR) are the largest family of cell surface Our results show that one specific subset of cross-docking simulations gave results of similar quality in advance of docking or receptor conformational adjustment after docking are more likely to produce substantial
- Dr. Nicola J. Smith - Dr. GPCR Podcast
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- Allosteric Effect of Nanobody Binding on Ligand-Specific Active States of the β2 Adrenergic Receptor
This activation is supported by the residues located at hotspots located on TMs 5, 6, and 7, as shown by supervised machine learning methods. Besides, ligand-specific subtle differences in the conformations assumed by intracellular loop 2 and
- Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall ...
After RNAi of HLGR2, distinct phenotypes were observed when HLGR2 expression was suppressed, indicating Conclusion: HLGR2 is essential for the growth and development and wing expansion and maturation in H. cunea, suggesting
- G-protein-coupled receptors as therapeutic targets for glioblastoma
Treatments include surgical resection, radiotherapy, and chemotherapy.
- A Chemical Biology Toolbox Targeting the Intracellular Binding Site of CCR9: Fluorescent Ligands ...
In a proof-of-principle study, we succeeded in showing that our CCR9-PROTAC is able to reduce CCR9 levels
- Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled ...
discovered that no single receptor drives this pattern, but rather multiple receptors contain amino acid substitutions Phenotypic characterization suggests these mutations induce perturbation of G protein activation and/ These data suggest that recurrent impactful oncogenic mutations perturb different GPCRs to subvert signaling and promote tumor growth or survival.
- HBx induces hepatocellular carcinogenesis through ARRB1-mediated autophagy to drive the G 1/S cycle
Arrb1 deficiency suppressed HBx-induced hepatocellular carcinogenesis in several mouse models. methyladenine or interference of ATG5 or ATG7 attenuated HBx-induced cell cycle acceleration and the subsequent hepatitis B virus X protein; HMGB1: high mobility group box 1; HIF1A/HIF-1α: hypoxia inducible factor 1 subunit NFKB/NF-κB: nuclear factor kappa B; PIK3CA: phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha; PIK3C3: phosphatidylinositol 3-kinase catalytic subunit type 3; PHHs: primary human hepatocytes
- Engineered synaptic tools reveal localized cAMP signaling in synapse assembly
We show that locally restricted suppression of postsynaptic cAMP levels or of cAMP-dependent protein-kinase In vivo, suppression of postsynaptic cAMP signaling in CA1 neurons prevented formation of both Schaffer-collateral and entorhinal-CA1/temporoammonic-path synapses, suggesting a general principle. Given that postsynaptic latrophilin adhesion-GPCRs drive synapse formation and produce cAMP, we suggest
- GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between ...
This communication involves the ligand-mediated control of cell surface receptors that then direct their Given the tremendous success of GPCRs as therapeutic targets, considerable focus has been placed on the ability of these therapeutics to modulate diseases by acting at cell surface receptors. In the past decade, however, attention has focused upon how stable multiprotein GPCR superstructures, termed receptorsomes, both at the cell surface membrane and in the intracellular domain dictate and
- GPCR voltage dependence controls neuronal plasticity and behavior
Thus, this study suggests that GPCR voltage dependency plays a role in many diverse neuronal functions
- A Model for the Signal Initiation Complex Between Arrestin-3 and the Src Family Kinase Fgr
Fgr SH3 domain at 1.9 Ã… resolution and developed a model for the GPCR-arrestin-3-Fgr complex that is supported This model suggests that Fgr interacts with arrestin-3 at multiple sites and is consistent with the locations
- Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled ..
Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed cells, macrophages, and in cardiovascular tissue, linking them to pseudo-allergic drug reactions and suggesting Consequently, the dynamic range for IL-6 detection as an assay for β-alanine-mediated activation of MRGPRD is substantially mediates the release of IL-6 in an in vitro system, hints at a role as an inflammatory mediator and supports
- G protein-coupled receptor interactions and modification of signalling involving the ghrelin ...
In vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors
- The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of ...
IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate
- In Vitro and In Silico Characterization of Kurarinone as a Dopamine D 1A Receptor Antagonist and ...
role of kurarinone, an abundant lavandulated flavonoid in Sophora flavescens , on dopamine receptor subtypes of the deep orthosteric binding pocket and the extracellular loops of D1R, D2LR, and D4R, validating substantial
- Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembra
The data support the inference that they act at the active interface between both transmembrane domains , the binding site involving residues of the TM6s of the GABAB1 and the GABAB2 subunit.
- Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage...
neonatal knockout mice for TASK1 ( task1 -/-) and TASK3 ( task3 -/-, the another highly expressed TASK subunit These outcomes suggest that LPA and several neurotransmitters impact MN IME via Gαi/o/Gαq-protein-coupled receptors, downstream ROCK2 activation, and subsequent inhibition of TASK1 channels.
- Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic ...
G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of a great variety
- G protein-coupled receptors that influence lifespan of human and animal models
GPCRs) may be a good option to try to prolong our life while maintaining good health since they have a substantial
- Chemical signaling regulates axon regeneration via the GPCR-Gqα pathway in Caenorhabditis elegans
Furthermore, the activating mutation in egl-30 encoding Gqα suppresses axon regeneration defective phenotype
- HDX-MS-optimized approach to characterize nanobodies as tools for biochemical and structural ...
The class IB PI3K, PI3Kγ, is a heterodimeric complex composed of a catalytic p110γ subunit bound to a p101 or p84 regulatory subunit.
- Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for ...
Implications for metabolic regulation G protein-coupled receptors (GPCRs) are a large family of cell surface
- Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin ...
This single point mutation in extracellular loop 2 of the β 2AR is sufficient to intrinsically bias the This study highlights the importance of extracellular control of intracellular response to stimuli and suggests
- Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial ...
with a concomitant decrease in the levels of cyclic adenosine monophosphate (cAMP), mRNA of manganese superoxide TGF-β1 stimulates the phosphorylation of Smad-3 and subsequent nuclear translocation to activate the
- Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas ...
Although most ORs were not ubiquitously expressed in gliomas, a subset of ORs displayed glioma subtype-specific Moreover, through systematic survival analysis on OR genes, OR51E1 (mouse Olfr558) was identified as a potential biomarker of unfavorable overall survival, and OR2C1 (mouse Olfr15) was identified as a potential biomarker of favorable overall survival in isocitrate dehydrogenase (IDH) wild-type glioma. this systematic analysis and review of the genomic and transcriptomic profiles of ORs in glioma, we suggest
- G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial ...
Furthermore, GRK2-knockdown ablated the sustained phase of endothelin-1 and angiotensin-II-stimulated Vasoconstrictor-stimulated phosphorylation of the Akt substrates GSK3α and GSK3β was ablated following These data suggest GRK2 expression is essential to facilitate vasoconstrictor-driven VSMC proliferation
- Melatonin MT 2 receptor is expressed and potentiates contraction in human airway smooth muscle
These findings suggest that the melatonin MT2 receptor is expressed in ASM, and modulates airway smooth