A5030865521- Chemical Synthesis and Analysis
- Neuropeptides and Animal Physiology
- Catalytic C–H Functionalization Methods
- Receptor Mechanisms and Signaling
- Click Chemistry and Applications
- Catalytic Cross-Coupling Reactions
- Synthesis and Biological Evaluation
- Hypothalamic control of reproductive hormones
- Synthesis and biological activity
- Chemical Synthesis and Reactions
- Synthesis and pharmacology of benzodiazepine derivatives
- Synthesis and Reactivity of Heterocycles
- HIV/AIDS drug development and treatment
- Alzheimer's disease research and treatments
- Synthesis of Organic Compounds
- Crystallization and Solubility Studies
- Synthesis and Catalytic Reactions
- Catalytic Alkyne Reactions
- Pharmacological Receptor Mechanisms and Effects
- X-ray Diffraction in Crystallography
- Phosphodiesterase function and regulation
- Computational Drug Discovery Methods
- Synthesis and Biological Activity
- Chemical synthesis and alkaloids
- Synthesis and Characterization of Heterocyclic Compounds
Université de Strasbourg
2016-2025
Centre National de la Recherche Scientifique
2015-2025
Laboratoire d'Innovation Thérapeutique
2016-2025
Institut Polytechnique de Bordeaux
2021-2025
Pharmac
2014-2021
Bipar
2015
Laboratoire de Biologie et Modélisation de la Cellule
2005-2007
Centre d’Immunologie de Marseille-Luminy
2001-2005
Institut de Biologie du Développement Marseille
2003-2005
Brigham and Women's Hospital
2004-2005
γ-Secretase is a structurally enigmatic multiprotein complex that catalyzes intramembrane proteolysis of variety substrates, including the amyloid β-protein precursor Alzheimer's disease and Notch receptor essential to cell differentiation. The active site this transmembrane aspartyl protease apparently lies at interface between two subunits presenilin-1 (PS1); however, evidence suggests existence an initial substrate-binding distinct from site. Here, we report photoaffinity probes based on...
A highly efficient, eco-friendly N-arylation was disclosed outspreading perspectives in green Buchwald–Hartwig reactions.
BACKGROUND AND PURPOSE Opiates remain the most effective compounds for alleviating severe pain across a wide range of conditions. However, their use is associated with significant side effects. Neuropeptide FF (NPFF) receptors have been implicated in several opiate‐induced neuroadaptive changes including development tolerance. In this study, we investigated consequences NPFF receptor blockade on acute and chronic stimulation opioid mice by using RF9, potent selective antagonist that can be...
Translocator protein 18 kDa (TSPO) is located in the mitochondrial outer membrane and plays an important role steroidogenesis cell survival.In central nervous system (CNS), its expression upregulated neuropathologies such as Alzheimer's disease (AD).Previously, we demonstrated that two new TSPO ligands based on imidazoquinazolinone termed 2a 2b, stimulated pregnenolone synthesis ATP production vitro.In present study, compared their effects to those of described literature (XBD173,...
Summary Multiple adaptations were necessary when plants conquered the land. Among them soluble phenylpropanoids related to plant protection and lignin for upright growth long‐distance water transport. Cytochrome P450 monooxygenase 98 ( CYP 98) catalyzes a rate‐limiting step in phenylpropanoid biosynthesis. Phylogenetic reconstructions suggest that single copy of founded each major land lineage (bryophytes, lycophytes, monilophytes, gymnosperms angiosperms), was maintained as all lineages but...
Starting from commercially available 2-chloro-3-hydroxypyridine, a new route leading to the first protypical pentaarylpyridine bearing five different substituents is reported. This strategy involves set of sequential but fully regiocontrolled Suzuki-Miyaura reactions and highlights 2-OBn pyridine protecting group as key intermediate. The played double role: (i) it allowed additional bromination at position 5 (ii) could afford reactive OTf species for last C-arylation step less hindered 2...
The design of bifunctional compounds is a promising approach toward the development strong analgesics with reduced side effects. We here report optimization previously published lead peptide KGFF09, which contains opioid receptor agonist and neuropeptide FF antagonist pharmacophores shown to induce potent antinociception evaluated novel hybrid peptides for their in vitro activity at MOP, NPFFR1, NPFFR2 selected four them (DP08/14/32/50) assessment acute antinociceptive mice. further DP32...
Abstract Opioid analgesics, such as morphine, oxycodone, and fentanyl, are the cornerstones for treating moderate to severe pain. However, on chronic administration, their efficiency is limited by prominent side effects analgesic tolerance dependence liability. Neuropeptide FF (NPFF) its receptors (NPFF1R NPFF2R) recognized an important pronociceptive system involved in opioid-induced hyperalgesia tolerance. In this article, we report design of multitarget peptidomimetic compounds that show...
Abstract Translocator protein 18 kDa (TSPO) is a mitochondrial located in the outer membrane and involved cholesterol translocation, prerequisite for steroid biosynthesis. TSPO modulation also appears to play role other functions, including respiration cell survival. In central nervous system, its expression up‐regulated neuropathology such as Alzheimer's disease (AD). Previously, we demonstrated that two new ligands, named 2a 2b, stimulated pregnenolone synthesis ATP production cellular...
An efficient and user-friendly palladium(II) precatalyst, POxAP (post-oxidative-addition precatalyst), was identified for use in Fukuyama cross-coupling reactions. Suitable storage under air, the precatalyst allowed reaction between thioesters organozinc reagents with turnover numbers of ∼90000. A series 23 ketones were obtained yields ranging from 53 to 99%. As proof efficacy, an alternative approach developed synthesis a key precursor natural product isoprekinamycin.
We previously demonstrated that the translocase protein TSPO2 together with voltage-dependent anion channel (VDAC) and adenine nucleotide transporter (ANT) were involved in a membrane transport complex human red blood cells (RBCs). Because VDAC was proposed as mediating ATP release RBCs, we used TSPO ligands ANT inhibitors to test this hypothesis. activated by ligands, blocked of ANT, while it insensitive pannexin-1 blockers. ligand increased extracellular (ATPe) concentration 24-59% over...
Abstract A copper‐catalyzed Ullmann‐type amination with primary amines in water a combination of copper(II) triflate [Cu(OTf) 2 ], dipivaloylmethane, and d ‐glucose is reported. The mild conditions the use an inexpensive catalyst as well renewable feedstock ( surfactant TPGS‐750‐M, which derived from vitamin E) make this protocol safe convenient strategy for efficient C−N bond formation. This easy‐to‐handle procedure extremely competitive compared to palladium‐based reactions may be used...
Abstract A simple, sustainable, efficient, mild, and low‐cost protocol was developed for d ‐glucose‐assisted Cu‐catalyzed Ullmann reactions in water amides, carbamates, nitrogen‐containing heterocycles. The reaction compatible with diverse aryl/heteroaryl iodides, giving highly substituted pyridine, indole, or indazole rings. This method offers an attractive alternative to existing protocols, because the proceeds aqueous media, occurs at near ambient temperature, provides N‐arylated products...
Aiming at advancing protocols for safer, environmentally sensible peptide synthesis we report our findings with regard to the occurrence of hydrogen cyanide (HCN, prussic acid) in amide bond-forming reactions mediated by diisopropylcarbodiimide (DIC) and ethyl (hydroxyimino)cyanoacetate (Oxyma). We determined that HCN is always formed on solid support N,N-dimethylformamide (DMF) when DIC/Oxyma employed. In an attempt minimize formation acid means preventing linear adduct 2 from cyclizing...
Carbon–nitrogen (C–N) bond‐forming cross‐coupling reactions catalyzed by palladium‐based systems, known as Buchwald–Hartwig aminations, are widely used in natural product synthesis, pharmaceuticals, agrochemicals, and materials science. However, these typically require organic solvents inert atmospheres, such argon, increasing environmental, health, safety (EHS) concerns. Using electron‐rich bulky phosphine ligands combination with [Pd(π‐cinnamyl)Cl]₂, we generate a highly active palladium...