A5025683789- Computational Drug Discovery Methods
- Genetics, Bioinformatics, and Biomedical Research
- Receptor Mechanisms and Signaling
- Advanced Biosensing Techniques and Applications
- Biotechnology and Related Fields
- Biosimilars and Bioanalytical Methods
- Cell Image Analysis Techniques
- Monoclonal and Polyclonal Antibodies Research
- Animal testing and alternatives
- Neuroendocrine regulation and behavior
- Neuropeptides and Animal Physiology
- Cell death mechanisms and regulation
- Molecular Biology Techniques and Applications
- Psidium guajava Extracts and Applications
- African Botany and Ecology Studies
- Mitochondrial Function and Pathology
- Nerve injury and regeneration
- Glioma Diagnosis and Treatment
- Viral Infectious Diseases and Gene Expression in Insects
- Physics and Engineering Research Articles
- Cancer, Hypoxia, and Metabolism
- thermodynamics and calorimetric analyses
- bioluminescence and chemiluminescence research
- interferon and immune responses
- Traditional and Medicinal Uses of Annonaceae
Université de Strasbourg
2014-2024
Centre National de la Recherche Scientifique
2014-2024
École Supérieure de Biotechnologie de Strasbourg
2014-2024
Institut Polytechnique de Bordeaux
2021-2022
Institut de Chimie des Substances Naturelles
2021
Université Paris-Saclay
2021
Laboratoire de Biophotonique et Pharmacologie
2020
Laboratoire d'Innovation Thérapeutique
2009-2020
Plateforme de chimie biologique intégrative de Strasbourg
2006-2020
Laboratoire des Biomolécules
2016
Among a small series of tested N-acylhydrazones (NAHs), the compound 8a was selected as selective submicromolar phosphodiesterase-4 (PDE4) inhibitor associated with anti-TNF-α properties measured both in vitro and vivo. The recognition pattern elucidated through molecular modeling studies based on knowledge 3D-structure zardaverine, PDE4 resembling structure 8a, cocrystallized PDE4. Based further conformational analysis dealing N-methyl-NAHs, quinazoline derivative (19) designed...
Polarity-sensitive fluorogenic dyes raised considerable attention because they can turn on their fluorescence after binding to biological targets, allowing background-free imaging. However, brightness is limited, and do not operate in the far-red region. Here, we present a new concept of dye based squaraine dimer that unfolds changing environment from aqueous organic thus turns its fluorescence. In media, all three newly synthesized dimers displayed short wavelength band characteristic an...
ABSTRACT Apoptosis, or programmed cell death, involves a cascade of regulatory events leading to the activation specific proteases. However, key substrates for these proteases remain be identified. We previously demonstrated that levels five unidentified polypeptides were specifically increased in neurons from embryonic chicken ciliary ganglia undergoing apoptosis by trophic deprivation. Here we show microsequencing two they are fragments actin. One them represents cleavage actin at site...
Abstract Classical fluorescence‐based approaches to monitor ligand–protein interactions are generally hampered by the background signal of unbound ligand, which must be removed tedious washing steps. To overcome this major limitation, we report here first red fluorescent turn‐on probes for a G protein‐coupled receptor (oxytocin receptor) at surface living cells. The peptide ligand carbetocin was conjugated one best solvatochromic (fluorogenic) dyes, Nile Red, turns on emission when reaching...
Oxytocin (OT) and its receptor (OT-R) are implicated in the etiology of autism spectrum disorders (ASD), OT-R is a potential target for therapeutic intervention. Very few nonpeptide oxytocin agonists have currently been reported. Their molecular vivo pharmacology remain to be clarified, none them has shown efficient improving social interaction animal models relevant ASD. In an attempt rationalize design centrally active full agonists, we studied systematic way structural determinants...
Herein, we show that a far-red arylidene-squaraine dye is stable against nucleophiles, in contrast to arene-squaraines. Owing the fluorescence enhancement apolar media together with high brightness and photostability, this was successfully applied detect oxytocin G protein-coupled receptor monitor its internalization living cells.
Background: The Balaruc-les-Bains’ thermal mud was found to be colonized predominantly by microorganisms, with cyanobacteria constituting the primary organism in microbial biofilm observed on surface. success of colonizing this specific ecological niche can explained part their taxa-specific adaptation capacities, and also diversity bioactive natural products that they synthesize. This array components has physiological properties may exploited for various applications. Methods: Nine...
We previously reported Chalcone-4 (1) that binds the chemokine CXCL12, not its cognate receptors CXCR4 or CXCR7, and neutralizes biological activity. However, this neutraligand suffers from limitations such as poor chemical stability, solubility, oral Herein, we report on discovery of pyrimidinone 57 (LIT-927), a novel CXCL12 which displays higher solubility than 1 is no longer Michael acceptor. While both reduce eosinophil recruitment in murine model allergic airway hypereosinophilia, only...
The local lipid microenvironment of transmembrane receptors is an essential factor in G protein coupled receptor (GPCR) signaling. However, tools are currently missing for studying endogenously expressed GPCRs primary cells and tissues. Here, we introduce fluorescent environment-sensitive GPCR ligands probing the living using fluorescence microscopy under no-wash conditions. We designed synthesized antagonist oxytocin (OTR) by conjugating a high-affinity nonpeptidic OTR ligand PF-3274167 to...
Cancer stem-like cells reside in hypoxic and slightly acidic tumor niches. Such microenvironments favor more aggressive undifferentiated phenotypes a slow growing "quiescent state" which preserves them from chemotherapeutic agents that essentially target proliferating cells. Our objective was to identify compounds active on glioblastoma cells, including under conditions mimick those found vivo within this most severe incurable form of brain malignancy. We screened the Prestwick Library...
We here describe a computational approach (POEM: Pocket Oriented Elaboration of Molecules) to drive the generation target-focused libraries while taking advantage all publicly available structural information on protein–ligand complexes. A collection 31 384 PDB-derived images with key shapes and pharmacophoric properties, describing fragment-bound microenvironments, is first aligned query target cavity by computer vision method. The fragments most similar PDB subpockets are then directly...
Current therapeutic treatments improving the impaired transportation of oxygen in acute respiratory distress syndrome (ARDS) have been found to be relevant and beneficial for treatment COVID-19 patients suffering from severe complications. Hence, we report preclinical preliminary results Phase I/II clinical trial LEAF-4L6715, a liposomal nanocarrier encapsulating kosmotropic agent trans-crocetin (TC), which, once injected, enhance oxygenation vascular tissue therefore has potential improve...
Abstract Excessive signaling by chemokines has been associated with chronic inflammation or cancer, thus attracting substantial attention as promising therapeutic targets. Inspired chemokine-clearing molecules shaped pathogens to escape the immune system, we designed a generic screening assay discover chemokine neutralizing (neutraligands) and unambiguously distinguish them from that block receptor (receptor antagonists). This assay, called TRIC-r, combines time-resolved intracellular...
(1) Background: Human exposure to organophosphorus compounds employed as pesticides or chemical warfare agents induces deleterious effects due cholinesterase inhibition. One therapeutic approach is the reactivation of inhibited acetylcholinesterase by oximes. While currently available oximes are unable reach central nervous system reactivate cholinesterases display a wide spectrum action against variety compounds, we aim identify new reactivators without such drawbacks. (2) Methods: This...
Abstract Osteosarcoma (OS) is the most common primary bone cancer, where overall 5‐year surviving rate below 20% in resistant forms. Accelerating cures for those poor outcome patients remains a challenge. Nevertheless, several studies of agents targeting abnormal cancerous pathways have yielded disappointing results when translated into clinic because lack accurate OS preclinical modeling. So, any effort to design drug testing may consider all inter‐, intra‐, and extra‐tumoral...
Ciliary neurotrophic factor (CNTF) has demonstrated therapeutic effects in several mouse mutants with motoneuronal degeneration. However, the poor bioavailability and toxic side of recombinant CNTF protein have complicated its use patients amyotrophic lateral sclerosis. gene transfer strategies were developed but faced question whether should be delivered to motoneuron cell bodies or their axons muscle targets. To address this issue, we used an adenoviral vector (AdCNTF) coding for a...
Background: Pediatric high-grade gliomas (pHGGs) are facing a very dismal prognosis and representative pre-clinical models needed for new treatment strategies. Here, we examined the relevance of collecting functional, genomic, metabolomics data to validate patient-derived in hypoxic microenvironment. Methods: From our biobank pediatric brain tumor-derived models, selected 11 pHGGs driven by histone H3.3K28M mutation. We compared features four patient tumors their paired cell lines mouse...