A5114949105- Neuropeptides and Animal Physiology
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Hypothalamic control of reproductive hormones
- Catalytic C–H Functionalization Methods
- Pharmacological Receptor Mechanisms and Effects
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Educational Methods and Media Use
- Analytical Chemistry and Chromatography
- Phenothiazines and Benzothiazines Synthesis and Activities
- Chemical Synthesis and Reactions
- Catalytic Cross-Coupling Reactions
- Metabolism and Genetic Disorders
- Signaling Pathways in Disease
- Tryptophan and brain disorders
- Breast Implant and Reconstruction
- Renal function and acid-base balance
- Biotin and Related Studies
- Carbohydrate Chemistry and Synthesis
- Lipoproteins and Cardiovascular Health
- Analytical Chemistry and Sensors
- Cancer Cells and Metastasis
- Cytokine Signaling Pathways and Interactions
- Cardiac Fibrosis and Remodeling
Université de Strasbourg
2012-2025
Laboratoire d'Innovation Thérapeutique
2015-2025
Centre National de la Recherche Scientifique
2012-2025
Institut Polytechnique de Bordeaux
2025
Institut de génétique et de biologie moléculaire et cellulaire
2017
Institut Clinique de la Souris
2017
Genopole (France)
2017
Kharkiv Medical Academy of Postgraduate Education
2016
Bipar
2015
Friedrich-Alexander-Universität Erlangen-Nürnberg
2015
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...
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...
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...
The effects of ciprofibrate (100 mg/d) on apolipoprotein (apo)B- and apoAI-containing lipoprotein subclasses, cholesteryl ester (CE) transfer protein activity, plasma high-density (HDL)-mediated cellular cholesterol efflux were evaluated in 10 patients displaying type IIB hyperlipidemia. Plasma concentrations large very low-density (VLDL)-1 (Sf 60–400) small VLDL-2 20–60) markedly diminished after fibrate treatment (−40%, P = 0.001; −25%, 0.003, respectively). We observed a reduction (−17%;...
Through the development of a new class unnatural ornithine derivatives as bioisosteres arginine, we have designed an orally active peptidomimetic antagonist neuropeptide FF receptors (NPFFR). Systemic low-dose administration this compound to rats blocked opioid-induced hyperalgesia, without any apparent side-effects. Interestingly, also observed that potentiated analgesia. This derivative provides novel therapeutic approach for both improving analgesia and reducing hyperalgesia induced by...
We report a selective ruthenium catalyzed reduction of tertiary amides on the side chain Fmoc-Gln-OtBu derivatives, leading to innovative unnatural α,β or γ-amino acids functionalized with amines. Rapid and scalable, this process allowed us build library basic amino at gram-scale directly usable for liquid- solid-phase peptide synthesis. The diversity available amines allows modulate physicochemical properties resulting acids, such as basicity hydrophobicity.
A series of dipeptides were designed as potential agonists the human KiSS1-derived peptide receptor (hGPR54). While sequence Arg-Trp-NH2 was most efficient in terms affinity, we established a convergent synthetic strategy to optimize N terminus. Using two successive Sonogashira cross-coupling reactions on solid-supported peptide, able introduce various alkynes at terminus afford compounds with sub-micromolar affinities for hGPR54. However, functional assays indicated benzoylated dipeptide...
RFamide-related peptide-3 (RFRP-3) and neuropeptide FF (NPFF) target two different receptor subtypes called FF1 (NPFF1R) FF2 (NPFF2R) that modulate several functions. However, the study of their respective role is severely limited by absence selective blockers. We describe here design a highly NPFF1R antagonist RF3286, which potently blocks RFRP-3-induced hyperalgesia in mice luteinizing hormone release hamsters. then showed pharmacological blockade prevents development fentanyl-induced...
Fifty-nine chronic schizophrenic patients received one year of treatment with either fluphenazine enanthate or pipothiazine palmitate IM. Both long acting neuroleptics significantly decreased serum albumin, total protein and creatinine values. Triglycerides were only early in treatment. Pretreatment findings from therapy responders, as compared those who failed to respond treatment, included higher albumin values a lesser extent, lower lactic dehydrogenase greater height. These results...
Herein, we report the diastereoselective synthesis of a 3-amino-1,2,4-oxadiazine (AOXD) scaffold. The presence N–O bond in ring prevents planar geometry aromatic system and induces strong decrease basicity guanidine moiety. While DIBAL-H appeared to be most efficient reducing agent because it exhibited high diastereoselectivity, observed various behaviors Mitsunobu reaction on resulting β-aminoalcohol, leading either inversion or retention configuration depending steric hindrance vicinity...
Abstract A chemical library is a key element in the early stages of pharmaceutical research. Its design encompasses various factors, such as diversity, size, ease synthesis, aimed at increasing likelihood success drug discovery. This article explores collaborative efforts computational and synthetic chemists tailoring libraries for cost‐effective resource‐efficient use, particularly context academic research projects. It proposes chemoinformatics methodologies that address two pivotal...
Abstract Translocator protein (TSPO, 18 kDa), previously known as peripheral-type benzodiazepine receptor, is an evolutionarily conserved membrane involved in various physiological processes and patho-physiological conditions. The endogeneous TSPO ligand a polypeptide of 9 kDa, but dipeptides with biological activity have been synthesized characterized. Herein, we phenyl alanine derived 19 F labelling which opens prospective for F-MRI potential F-PET applications. We characterized the...
Abstract Intramolecular Buchwald—Hartwig cyclization of 2‐bromophenylalanine derivatives allows the synthesis chiral dihydroquinolines (II).