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Results found for "Brigitte Kieffer"
- CD28 and chemokine receptors: Signalling amplifiers at the immunological synapse
To exert their functions requiring high sensibility and specificity, T cells need to integrate different
- Viral G Protein-Coupled Receptors Encoded by β- and γ-Herpesviruses
We discuss ligand binding, signaling, and structures of the vGPCRs in light of robust differences from
- Community guidelines for GPCR ligand bias: IUPHAR review 32
Depending on which ligand activates a receptor, it can engage different intracellular transducers.
- Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84
and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing using ligands with differing
- Molecular insights into regulation of constitutive activity by RNA editing 5HT2C serotonin receptor
These 5HT2C isoforms display differences in constitutive activity, agonist/inverse agonist potencies,
- Endogenous ligand recognition and structural transition of a human PTH receptor
The distinct molecular actions are ascribed to the differences in ligand recognition and dissociation
- The complicated lives of GPCRs in cardiac fibroblasts
October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system
- Hear the sounds: the role of G protein-coupled receptors in the cochlea
protein-coupled receptors (GPCRs) are crucial receptors that regulate a wide range of physiological functions in different
- Fusion protein strategies for cryo-EM study of G protein-coupled receptors
Here, we address this shortcoming by exploring different fusion protein designs, which lead to structures
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
The choice of pathway can result in different cellular responses, underscoring the criticality of precise several high-throughput screening (HTS) assays for ERK activation have been developed, each utilising different
- GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin...
receptors "Serotonin (or 5-hydroxytryptamine, 5-HT) is an important neurotransmitter that activates 12 different
- A central alarm system that gates multi-sensory innate threat cues to the amygdala
Previous findings suggest that parallel pathways independently relay innate threat signals from different
- Endogenous ligand recognition and structural transition of a human PTH receptor
The distinct molecular actions are ascribed to the differences in ligand recognition and dissociation
- Pharmacology at Your Fingertips: Terry’s Corner Launches
Distinct Ligand Activation in NMBR Simulations show how two ligands differently activate class A GPCR
- Allosteric modulation of GPCRs: From structural insights to in silico drug discovery
Recent advances in the structure determination of GPCRs bound to different types of allosteric modulators
- Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of...
The observed differences in the binding affinity and cooperativity arise from the functional groups that
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
versatile molecular tools to study G protein-coupled receptors (GPCRs) and can be used for a range of different
- Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery
site-directed) approaches, mutagenesis can provide a comprehensive understanding of how drugs interact with different Furthermore, probing species- or subtype-selectivity introduces complexities due to the differing contexts
- Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes
Likewise, the relative importance of receptor activation state and ligand function differences have also The distributions of ligand RMSD values were not statistically different for these two conditions, according
- Helix 8 in chemotactic receptors of the complement system
By comparing two C5aR receptors C5aR1 and C5aR2 we explained differences between their signaling pathways
- Lipid Modulation of a Class B GPCR: Elucidating the Modulatory Role of PI(4,5)P 2 Lipids
This suggests differences in the regulatory function of PI(4,5)P2 between class A and class B GPCRs."
- Ligands can differentially and temporally modulate GPCR interaction with 14-3-3 isoforms
Multiple 14-3-3 isoforms exist, and a GPCR can differentially interact with different 14-3-3 isoforms
- Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its...
and described interactions within its key regions and the bounded ligands to identify their notable differences
- TRPM3 in the eye and in the nervous system - from new findings to novel mechanisms
TRPM3 expression patterns differ between species and change during development.
- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
September 2022 "The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different
- The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
Several recent studies have demonstrated that TGR5 exerts inconsistent effects in different cancer cells
- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
It has been applied to different GPCR binding assays, such as CXCR4, opioid receptors, CCK1 and CCK2. Discussion The saturation experiments revealed a lower 2-fold difference in the Kd for each CBR receptor A graphic highlighting these differences can be found in Figure 7 . Figure 7. It highlights the difference in affinity of compounds such as SCRAs and other synthetic cannabinoids. Indeed, the difference is lower than 1pKi value between both experiments.
- Discovery of 3(2-aminoethyl)-thiazolidine-2,4-diones as a novel chemotype of sigma-1 receptor ligand
We have explored hydrophobic groups of different sizes on both sides of the five-membered ring scaffold
- Synaptic integration of subquantal neurotransmission by co-localized G protein coupled receptors in
Colocalization of different actions of GPCRs provide synaptic integration within presynaptic terminals Their effects are profoundly different.
- 📰 GPCR Weekly News, June 26 to July 2, 2023
dairy fat biomarker, stimulates insulin secretion and activates G protein-coupled receptors with a different GPCRs in Neuroscience Fine-tuning GPCR-mediated neuromodulation by biasing signaling through different



