A5076786364- Monoclonal and Polyclonal Antibodies Research
- Receptor Mechanisms and Signaling
- Immune Response and Inflammation
- Antimicrobial Peptides and Activities
- Computational Drug Discovery Methods
- Adenosine and Purinergic Signaling
- Chemokine receptors and signaling
- Influenza Virus Research Studies
- Advanced Biosensing Techniques and Applications
- Axon Guidance and Neuronal Signaling
- interferon and immune responses
- Protein Kinase Regulation and GTPase Signaling
- Phagocytosis and Immune Regulation
- Glycosylation and Glycoproteins Research
Inserm
2021-2024
Université de Montpellier
2021-2024
Centre National de la Recherche Scientifique
2021-2024
Institut de Génomique Fonctionnelle
2022-2024
University of Nottingham
2020
University of Birmingham
2020
Atypical Chemokine Receptor 3 (ACKR3) belongs to the G protein-coupled receptor family but it does not signal through proteins. The structural properties that govern functional selectivity and conformational dynamics of ACKR3 activation are poorly understood. Here, we combined hydrogen/deuterium exchange mass spectrometry, site-directed mutagenesis, molecular simulations examine binding mode mechanism action ligands different efficacies. Our results show or inhibition is governed by...
Abstract To study the localisation of G protein-coupled receptors (GPCR) in their native cellular environment requires visualisation through fluorescent labelling. overcome requirement for genetic modification receptor or limitations dissociable ligands, here we describe rational design a compound that covalently and selectively labels GPCR living cells with moiety. We designed antagonist, which linker incorporated between pharmacophore (ZM241385) fluorophore (sulfo-cyanine5) is able to...
Staphylococcus aureus (SA) leukocidin ED (LukED) belongs to a family of bicomponent pore forming toxins that play important roles in SA immune evasion and nutrient acquisition. LukED targets specific G protein-coupled chemokine receptors lyse human erythrocytes (red blood cells) leukocytes (white cells). The first recognition step is critical for cell targeting lysis. structural molecular bases this mechanism are not well understood but could constitute essential information guide antibiotic...
Abstract Atypical Chemokine Receptor 3 (ACKR3) is a G protein-coupled receptor that does not signal through proteins. It known as chemokine scavenger involved in various pathologies, making it an appealing yet intriguing therapeutic target. Indeed, the structural properties govern ACKR3 functional selectivity and overall conformational dynamics of activation are poorly understood. Here we combined Hydrogen/Deuterium exchange mass spectrometry (HDX-MS) molecular simulations to examine binding...
Abstract Chemokine receptor 4 (CXCR4) is a member of the chemokine exclusively activated by CXCL12. While CXCR4 regulates numerous physiological processes associated with cell migration and embryogenesis, its overexpression has been involved in various cancer types. Studies suggest that intracellular expression rather than CXCR4-operated signaling underlies pro-tumorigenic functions. Given role GPCR interacting proteins their trafficking subcellular localization, we characterized interactome...
Abstract Chemokine stimulation of atypical chemokine receptor 3 (ACKR3) does not activate G proteins but recruits arrestins. It is a scavenger that indirectly influences responses by restricting the availability CXCL12, an agonist shared with canonical CXCR4. ACKR3 upregulated in numerous disorders. Due to limited insights chemokine-activated signaling, it unclear how contributes pathological phenotypes. One explanation may be high constitutive activity drives non-canonical signaling through...
Abstract Here, we describe rational design of a compound that covalently and selectively labels G protein-coupled receptor (GPCR) in living cells with fluorescent moiety. Using wild-type adenosine A 2A as model system, show labelling without impeding access to the orthosteric binding site demonstrate its use endogenously expressing systems. This offers non-invasive selective approach study function localisation native GPCRs.
Abstract Staphylococcus aureus (SA) leukocidin LukED belongs to a family of bicomponent pore forming toxins that play important roles in SA immune evasion and nutrient acquisition. targets specific G protein-coupled chemokine receptors lyse human erythrocytes leukocytes. The first recognition step is critical for cell targeting lysis. structural molecular bases this mechanism are not well understood but could constitute essential information guide antibiotic development. Here, we...