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308 items found for "Single-cell transcriptome"
- Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin...
Here, we discovered that the epithelial-cell-derived antimicrobial peptides defensins activated orphan
- 📰 GPCR Weekly News, July 17 to July 23, 2023
Submit a 1-minute abstract video and tell us more about your project in this form. Drosophila homologue of mammalian adhesion GPCRs, is involved in antitumor reactions to injected oncogenic cells GPCRs in Oncology and Immunology A GPCR checkpoint drives CD8+ T cell dysfunction and immunotherapy failure
- Drug Discovery Picks Up the Pace, Stays on Target
small molecules that conditionally modulate proteins in their functional state; three-dimensional (3D) cell
- Targeting Intracellular Allosteric Sites in GPCRs
Exploring the intracellular allosteric site GPCRs represent one of the largest and most vital families of cell hand, selectivity could be achieved by merging both orthosteric and allosteric pharmacophores within a single
- Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its...
They participate in the activation, chemotaxis and recruitment of multiple immunological cells such as
- Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of...
nab-paclitaxel has shown clinical activity in advanced TNBC with PD-L1-positive tumor-infiltrating immune cells
- Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System
vary between antagonist, partial agonist, and biased agonist outcomes in various primary and clonal cell We will discuss the historic context of pepducin development for each receptor, as well as the structural
- Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated
Here we investigated a potential mechanism for regulation of PLC signaling downstream of MOR in HEK293 cells
- 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 cells
- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
S1P5 is predominantly expressed in nervous and immune systems, regulating the egress of natural killer cells from lymph nodes and playing a role in immune and neurodegenerative disorders, as well as carcinogenesis
- Biased Agonism at the GLP-1 Receptor: A Pathway to Improved Therapeutic Outcomes
integral to metabolic regulation, particularly in glucose homeostasis and insulin secretion, making it a well-established Cell Metab, 2018. 27 (4): p. 740-756. 3. Cell, 2016. 165 (7): p. 1632-1643. 6.
- A Setmelanotide-like Effect at MC4R Is Achieved by MC4R Dimer Separation
interaction were conducted, confirming decreased homodimerization capacities of chimeric receptors in HEK293 cells
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal...
transduce signals across the plasma membrane and orchestrate a multitude of physiological processes within cells
- Pharmacological Properties and Function of PxOctβ3 Octopamine Receptor in Plutella xylostella (L.)
This ORF was also cloned and expressed in HEK-293 cells.
- Molecular basis for variations in the sensitivity of pathogenic rhodopsin variants to 9-cis-retinal
previously uncharacterized variants, that exhibit diminished plasma membrane expression in HEK293T cells
- 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
- 📰 GPCR Weekly News, January 30 to February 5, 2023
expansion to enable site-specific bioorthogonal labeling of functional G protein-coupled receptors in live cells activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell Discovery Upstream Bio Announces the Appointment of Marcella Ruddy, M.D., to the Board of Directors Call
- 📰 GPCR Weekly News, January 8 to 14, 2024
her team studied the GPER/GPR30 complex with β1-adrenergic receptor and AKAP5 in MCF7 breast cancer cells kinase (MAGUK) scaffold protein, and protein kinase A anchoring protein (AKAP) 5 in MCF7 breast cancer cells
- Precise druggability of the PTH type 1 receptor
selective small molecules with strong negative allosteric and biased properties for PTHR signaling in cell
- Therapeutic validation of an orphan G protein‐coupled receptor
process of de-orphanizing, is of great importance in order to better understanding human physiology as well GPR84 is a Gi‐coupled class A GPCR mainly expressed in immune cells and microglia in the brain (Wojciechowicz Regarding the first question, GPR84 overexpression in immune cells in a range of pro‐inflammatory disorders in respect to tool compounds to study the function of this receptor towards clinical validation, as well In addition, several GPR84 ligands have been described as well as GPR84 knockout mice.
- A Chemical Biology Toolbox Targeting the Intracellular Binding Site of CCR9: Fluorescent Ligands ...
first synthesized a fluorescent ligand enabling equilibrium and kinetic binding studies via NanoBRET as well Applying this molecular tool in a membrane-based setup and in living cells, we discovered a 4-aminopyrimidine
- Structure Therapeutics Extends Financing, Advances Diabetes and Obesity Clinical Program and...
In addition, Structure Therapeutics has completed dosing in a single ascending dose (SAD) Phase 1 study
- Overview of adhesion GPCRs self-activation
Last month a very detailed paper analyzed the molecular mechanisms of the aGPCRs self-activation as well self-activation of aGPCRs, some of which differ from those of GPCRs belonging other families, and I will tell Through cell-based assays and Cryo-EM of high quality, it was possible to know that ADGRL3 can activate Araç, D., et al., A novel evolutionarily conserved domain of cell-adhesion GPCRs mediates autoproteolysis Molecular cell, 82(22), 4340–4352.e6.
- Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental...
endoplasmic reticulum stress, dysregulated immune tolerance, vascular inflammation and endothelial cell
- 📰 GPCR Weekly News, November 20 to 26, 2023
structural conservation across distant species Industry News Avantor's (AVTR) New Offerings to Aid Cell and Gene Therapy Suite Avantor® Expands Cellular Science Offerings with Multispan Cell Engineering and
- C5aR2 receptor: The genomic twin of the flamboyant C5aR1
classical G-protein-coupled receptor (GPCR), whereas C5aR2 is a nonclassical GPCR that tailors immune cell
- 📰 GPCR Weekly News, April 15 to 21, 2024
Kv7 channels via Gi/o protein signalling and modulates excitability of human induced pluripotent stem cell-derived Updates in GPCR Research Alared: Solvatochromic and Fluorogenic Red Amino Acid for Ratiometric Live-cell
- Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild trauma
effect of Ang-(1-7) on secondary injury observed in a murine model of mild TBI (mTBI) in a closed skull, single