A5034830803- HIV Research and Treatment
- HIV/AIDS drug development and treatment
- Protein Structure and Dynamics
- Fluorine in Organic Chemistry
- Chemical Synthesis and Analysis
- Glycosylation and Glycoproteins Research
- Analytical Chemistry and Chromatography
- Carbohydrate Chemistry and Synthesis
- Mass Spectrometry Techniques and Applications
- Cancer-related gene regulation
- Cholinesterase and Neurodegenerative Diseases
- Antibiotic Resistance in Bacteria
- Dendrimers and Hyperbranched Polymers
- Crystallization and Solubility Studies
- Genomics, phytochemicals, and oxidative stress
- Click Chemistry and Applications
- Computational Drug Discovery Methods
- Synthesis and Reactivity of Heterocycles
- Bacterial Genetics and Biotechnology
- Synthesis and Characterization of Heterocyclic Compounds
- Redox biology and oxidative stress
- RNA Interference and Gene Delivery
- Amino Acid Enzymes and Metabolism
- Nicotinic Acetylcholine Receptors Study
- RNA and protein synthesis mechanisms
Université de Rouen Normandie
2010-2022
Laboratoire COBRA
2011-2022
Normandie Université
2013-2022
Centre National de la Recherche Scientifique
2010-2022
Institut National des Sciences Appliquées Rouen Normandie
2010-2022
Génétique Moléculaire Génomique Microbiologie
2004-2021
Différenciation et Communication Neuronale et Neuroendocrine
2016
Délégation Paris 5
2002-2006
Université Paris Cité
2002-2006
Inserm
2003-2006
ObjectivesIn the context of increasing worldwide occurrence imipenem-resistant Acinetobacter baumannii strains, we investigated a possible porin-mediated mechanism relating to carbapenem resistance-associated outer membrane protein, CarO. The aim this study was determine whether porin may be diffusion pathway for carbapenems in A. baumannii.
This study was undertaken to characterize functions of the outer membrane protein OmpW, which potentially contributes development colistin‐ and imipenem‐resistance in Acinetobacter baumannii . Reconstitution OmpW artificial lipid bilayers showed that it forms small channels (23 pS 1 m KCl) markedly interacts with iron colistin, but not imipenem. In vivo, 55 Fe uptake assays comparing behaviours Δ ompW mutant wild‐type strains confirmed a role for A. homeostasis. However, loss expression did...
To replicate, human immunodeficiency virus, type 1 (HIV-1) needs to integrate a cDNA copy of its RNA genome into chromosome the host cell, step controlled by viral integrase (IN) protein. Viral integration involves participation several cellular proteins. SNF5/Ini1, subunit SWI/SNF chromatin remodeling complex, was first cofactor identified interact with IN. We report here that SNF5/Ini1 interferes early steps HIV-1 replication. Inhibition expression interference increases Using quantitative...
The aim of this work was to develop a reliable and efficient analytical method characterise differentiate saxitoxin analogues (STX), including sulphated (gonyautoxins, GTX) non-sulphated analogues. For purpose, hydrophilic interaction liquid chromatography (HILIC) used separate We also resorted ion mobility spectrometry the STX because technique adds new dimension separation based on gas phase conformation. Positive negative ionisation modes were for gonyautoxins while positive mode...
A protein−protein association regulated by phosphorylation of serine is examined NMR studies. Degradation the HIV receptor CD4 proteasome, mediated HIV-1 protein Vpu, crucial for release fully infectious virions. Phosphorylation Vpu at two sites, Ser52 and Ser56, on motif DSGXXS required interaction with ubiquitin ligase SCF-βTrCP which triggers degradation proteasome. This conserved in several signaling proteins known to be degraded To elucidate basis β-TrCP recognition, bound conformation...
Synthesis of fluorocyclopropyl building blocks, which constitute the core various therapeutic agents against hepatitis C virus, is described. The relevant methyl α-amino-β-fluoro-β-vinylcyclopropanecarboxylate has been used as a key intermediate for total synthesis fluorinated analogue Simeprevir (TMC 435), HCV NS3/4A protease inhibitor.
We reported the use of ion mobility (IM) combined with mass spectrometry (MS) as an analytical tool to investigate low generation polyamidoanine (PAMAM) dendrimers. This approach has been employed separate ions defective structures different charge state but exactly same m/z value. Tandem (MS/MS) after IM separation allowed a comprehensive structural characterization In addition, was used evaluate collision cross-sections perfect They showed good correlation calculated obtained by trajectory...
Abstract: Recently, it has been shown that mammalian PEBPs are implicated in several signalling pathways controlling the cellular cycle. In particular, during brain development, N‐terminal part of PEBP is specifically cleaved and resulting 11 amino acid peptide stimulates growth activity acetylcholinergic neurons. The crystallographic structure bovine human revealed their N‐ C‐terminal parts accessible exposed to solvent suggesting they may be involved specific interactions with partners. We...
beta-TrCP is the F-box protein component of an Skp1/Cul1/F-box (SCF)-type ubiquitin ligase complex. Biochemical studies have suggested that targets oncogenic beta-catenin for ubiquitination and followed by proteasome degradation. To further elucidate basis this interaction, a complex between 32-residue peptide from containing phosphorylated motif DpSGXXpS (P-beta-Cat17-48) was studied using Saturation Transfer Difference (STD) Nuclear Magnetic Resonance (NMR) experiments. These experiments...
Thioglycosides, even if rare in Nature, have gained increased interest for their biological properties. Chemical syntheses of this class compounds been largely studied but little has reported on biosynthesis. Herein, combining experiments from the different fields enzymology, bioorganic chemistry and molecular modeling, we wish to demonstrate versatility glucosyltransferase UGT74B1 its synthetic potency preparation a variety natural unnatural desulfoglycosinolates.
We previously characterized a set of potent pseudo-irreversible inhibitors acetylcholinesterase (AChE) based on redox prodrug strategy. Among the various synthesized prodrugs, compound 1, namely DQS1-02, displayed favorable physicochemical properties and was chosen to achieve necessary prerequisite investigations prior preclinical evaluation. Herein, we first report practical multigram-scale nine-step synthesis 1 with good overall yield (18%) as well full investigation inhibition mechanism...
We present here the preparation and structural characterization of first-generation ammonia-cored polyamidoamine (PAMAM) dendrimers modified with glycine residues. Chemical modification dendrimer was done to increase biocompatibility these compounds, known be effective delivery agents for drugs or genes. Fully PAMAM [Gly6G1(N)] on one hand partially [GlynG1(N), n = 0 6)] other were obtained depending experimental conditions. The resulting have cautiously characterized understand interpret...
Over the years, numerous modifications to structure of proline have been made in order tune its effects on bioactive compounds. Notably, introduction a cyclopropane ring or fluorine atom has produced interesting results. Herein, we describe synthesis containing fluorocyclopropane. This modified amino acid was inserted into tripeptide, whose conformation studied by nuclear magnetic resonance and density functional theory calculations.
With the aim of repositioning commercially available drugs for inhibition anti-apoptotic myeloid cell leukemia protein, Mcl-1, implied in various cancers, five molecules, highlighted from a published theoretical screening, were selected to experimentally validate their affinity toward Mcl-1. A detailed NMR study revealed that only two tested drugs, Torsemide and Deferasirox, interacted with data analysis allowed complete characterization binding mode both including estimation Biological...
The conformational preferences of a 22-amino acid peptide (LIDRLIERAEDpSGNEpSEGEISA) that mimics the phosphorylated HIV-1-encoded virus protein U (Vpu) antigen have been investigated by NMR spectroscopy. Degradation HIV receptor CD4 proteasome, mediated HIV-1 Vpu, is crucial for release fully infectious virions. Phosphorylation Vpu at sites Ser52 and Ser56 on DSGXXS motif required interaction with ubiquitin ligase SCFβ-TrCP which triggers degradation proteasome. This conserved in several...