A5040367251- Connexins and lens biology
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Supramolecular Self-Assembly in Materials
- Biochemical effects in animals
- Nicotinic Acetylcholine Receptors Study
- Chemical Synthesis and Analysis
- Biochemical Analysis and Sensing Techniques
- Regulation of Appetite and Obesity
- Genetics, Aging, and Longevity in Model Organisms
- Synthetic Organic Chemistry Methods
- Receptor Mechanisms and Signaling
- RNA Interference and Gene Delivery
- Dendrimers and Hyperbranched Polymers
- Polymer composites and self-healing
- Crystallography and molecular interactions
- Carbon dioxide utilization in catalysis
- Computational Drug Discovery Methods
- COVID-19 Clinical Research Studies
- Adipose Tissue and Metabolism
- Lipid Membrane Structure and Behavior
- Human Health and Disease
- biodegradable polymer synthesis and properties
- Heme Oxygenase-1 and Carbon Monoxide
- Neuropeptides and Animal Physiology
Vrije Universiteit Brussel
2020-2024
Université de Bordeaux
2017-2024
Institut Polytechnique de Bordeaux
2017-2024
Centre National de la Recherche Scientifique
2017-2024
Laboratoire de Chimie des Polymères Organiques
2024
Institut Européen de Chimie et Biologie
2017
The helix, turn, and β-strand motifs of biopolymer folded structures have been found to prevail also in non-natural backbones. In contrast, foldamers with aryl rings their main chains possess distinct conformations that may give access objects beyond the reach peptidic nucleotidic search such original architectures, we explored effect bending aromatic amide β-sheets using building blocks impart curvature. Cyclic multiturn noncyclic sequences were synthesized, characterized solution solid...
Melanocortin 4 receptor (MC4-R) antagonists are actively sought for treating cancer cachexia. We determined the structures of complexes with PG-934 and SBL-MC-31. These peptides differ from SHU9119 by substituting His6 Pro6 inserting Gly10 or Arg10. The revealed two subpockets at TM7-TM1-TM2 domains, separated N2857.36. Two peptide series based on complexed led to an antagonist activity selectivity SAR study. Most ligands retained potency, but several SBL-MC-31-derived significantly enhanced...
A vanillin monomer featuring a carbonate linkage in its center was synthesized and used to prepare degradable biobased polymer networks.
Pannexin1 channels facilitate paracrine communication and are involved in a broad spectrum of diseases. Attempts to find appropriate pannexin1 channel inhibitors that showcase target-selective properties vivo applicability remain nonetheless scarce. However, promising lead candidate, the ten amino acid long peptide mimetic 10Panx1 (H-Trp1-Arg2-Gln3-Ala4-Ala5-Phe6-Val7-Asp8-Ser9-Tyr10-OH), has shown potential as inhibitor both vitro studies. Nonetheless, structural optimization is critical...
Following a rational design, series of macrocyclic ("stapled") peptidomimetics 10Panx1, the most established peptide inhibitor Pannexin1 (Panx1) channels, were developed and synthesized. Two analogues SBL-PX1-42 SBL-PX1-44 outperformed linear native peptide. During in vitro adenosine triphosphate (ATP) release Yo-Pro-1 uptake assays Panx1-expressing tumor cell line, both compounds revealed to be promising bidirectional inhibitors Panx1 channel function, able induce two-fold inhibition, as...
The melanocortin receptors (MC1R-MC5R) belong to class A G-protein-coupled (GPCRs) and are known have receptor-specific roles in normal diseased states. Selectivity for MC4R is of particular interest due its involvement various metabolic disorders, including obesity, feeding regulation, sexual dysfunctions. To further improve the potency selectivity (ant)agonist peptide ligands, we designed synthesized a series cyclic peptides based on recent crystal structure complex with well-characterized...
A peptide segment that is 10 residues long at the C-terminal (CT) region of Cx43 known to be involved in interactions, both with protein itself and other proteins, result hemichannel (HC) activity regulation. Previously reported mimetic peptides based on this (e.g., αCT1, CT10) have been revealed promising therapeutic agents context cardiovascular diseases. In work, novel approaches, such as C- N-terminal modification cyclization, improve proteolytic stability bioavailability CT10 are...
Although many efforts have been made to elucidate the pathogenesis of COVID-19, underlying mechanisms are yet be fully uncovered. However, it is known that a dysfunctional immune response and accompanying uncontrollable inflammation lead troublesome outcomes in COVID-19 patients. Pannexin1 channels put forward as interesting drug targets for treatment due their key role link other viral infections. In present study, we selected panel drugs previously tested clinical trials potential...
Pannexin1 channels facilitate paracrine communication and are involved in a broad spectrum of diseases. Despite an increasing interest these over the past few years, attempts to find appropriate channel inhibitors that showcase target selective properties vivo applicability scarce. However, promising lead candidate, ten amino acid long peptide mimetic 10Panx1 (H-Trp1-Arg2-Gln3-Ala4-Ala5-Phe6-Val7-Asp8-Ser9-Tyr10-OH), has shown promise as inhibitor both vitro studies. structural optimization...