A5021383328- Circadian rhythm and melatonin
- Receptor Mechanisms and Signaling
- Free Radicals and Antioxidants
- Chemical Synthesis and Analysis
- Neuropeptides and Animal Physiology
- Regulation of Appetite and Obesity
- Monoclonal and Polyclonal Antibodies Research
- Photoreceptor and optogenetics research
- Pharmacogenetics and Drug Metabolism
- Protein Kinase Regulation and GTPase Signaling
- Biochemical Analysis and Sensing Techniques
- Neurobiology and Insect Physiology Research
- Coenzyme Q10 studies and effects
- Peroxisome Proliferator-Activated Receptors
- Adipose Tissue and Metabolism
- Genomics, phytochemicals, and oxidative stress
- Neuroendocrine regulation and behavior
- Bioactive Compounds and Antitumor Agents
- Neurotransmitter Receptor Influence on Behavior
- Neuroscience and Neuropharmacology Research
- Computational Drug Discovery Methods
- Analytical Chemistry and Chromatography
- Fibroblast Growth Factor Research
- Pancreatic function and diabetes
- Protein Tyrosine Phosphatases
Inserm
2007-2024
Université de Rouen Normandie
2007-2024
Institut des Hautes Études Scientifiques
2012-2023
Servier (France)
2014-2023
Magna Graecia University
2018-2023
Université Toulouse III - Paul Sabatier
2014-2023
Institut de Recherche pour le Développement
2014-2023
Université de Toulouse
2018-2023
Différenciation et Communication Neuronale et Neuroendocrine
2021-2023
Institute for International Social Research
2019-2023
The regulation of the circadian rhythm is relayed from central nervous system to periphery by melatonin, a hormone synthesized at night in pineal gland. Besides two melatonin G-coupled receptors, mt<sub>1</sub> and MT<sub>2</sub>, existence novel putative receptor,<i>MT<sub>3</sub></i> , was hypothesized observation binding site both peripheral hamster tissues with an original profile very rapid kinetics ligand exchange compared MT<sub>2</sub>. In this report, we present purification...
Because little comparative information is available concerning receptor profiles of antiparkinson drugs, affinities 14 agents were determined at diverse receptors implicated in the etiology and/or treatment Parkinson9s disease: human (h)D<sub>1</sub>, hD<sub>2S</sub>, hD<sub>2L</sub>, hD<sub>3</sub>, hD<sub>4</sub>, and hD<sub>5</sub> receptors; 5-hydroxytryptamine (5-HT)<sub>1A</sub>, h5-HT<sub>1B</sub>, h5-HT<sub>1D</sub>, h5-HT<sub>2A</sub>, h5-HT<sub>2B</sub>,...
The principal soy phytoestrogen genistein has an array of biological actions. It binds to estrogen receptor (ER) α and β ER-mediated estrogenic effects. In addition, it antiestrogenic effects as well non-ER-mediated such inhibition tyrosine kinase. Because its complex actions, the molecular mechanisms action are poorly understood. Here we show that dose-dependently increases transcriptional activity in mesenchymal progenitor cells, but on osteogenesis adipogenesis different. At low...
Our group has recently demonstrated (Gesta, S., Simon, M., Rey, A., Sibrac, D., Girard, Lafontan, Valet, P., and Saulnier-Blache, J. S. (2002) Lipid Res. 43, 904-910) the presence, in adipocyte conditioned-medium, of a soluble lysophospholipase d-activity (LPLDact) involved synthesis bioactive phospholipid lysophosphatidic acid (LPA). In present report, LPLDact was purified from 3T3F442A adipocyte-conditioned medium identified as type II ecto-nucleotide pyrophosphatase phosphodiesterase,...
Ligand-target residence time is emerging as a key drug discovery parameter because it can reliably predict efficacy in vivo. Experimental approaches to binding and unbinding kinetics are nowadays available, but we still lack reliable computational tools for predicting time. Most attempts have been based on brute-force molecular dynamics (MD) simulations, which CPU-demanding not yet particularly accurate. We recently reported new scaled-MD-based protocol, showed potential prediction...
G protein-coupled receptors (GPCRs) are integral membrane proteins that play a pivotal role in signal transduction. Understanding their dynamics is absolutely required to get clear picture of how signaling proceeds. Molecular characterization GPCRs isolated detergents nevertheless stumbles over the deleterious effect these compounds on receptor function and stability. We explored here potential styrene-maleic acid polymer solubilize directly from lipid environment. To this end, we used two...
Herein, we evaluate the interaction of α2-AR antagonist, yohimbine, as compared to fluparoxan, at multiple monoaminergic receptors and examine their roles in modulation adrenergic, dopaminergic serotonergic transmission freely-moving rats. Yohimbine displays marked affinity human (h)α2A-, hα2B- hα2C-ARs, significant for h5-HT1A, h5-HT1B, h5-HT1D, hD2 weak hD3 receptors. In [35S]GTPγS binding protocols, yohimbine exerts antagonist actions hα2A-AR, sites, yet partial agonist h5-HT1A sites....
The daily rhythm in melatonin levels is controlled by cAMP through actions on the penultimate enzyme synthesis, arylalkylamine N -acetyltransferase (AANAT; serotonin -acetyltransferase, EC 2.3.1.87 ). Results presented here describe a regulatory/binding sequence AANAT that encodes cAMP-operated binding switch which cAMP-regulated protein kinase-catalyzed phosphorylation [RRHTLPAN → RRHpTLPAN] promotes formation of complex with 14-3-3 proteins. Formation this AANAT/14-3-3 enhances production...
The accompanying multivariate analysis of the binding profiles antiparkinson agents revealed contrasting patterns affinities at diverse classes monoaminergic receptor. Herein, we characterized efficacies human (h)D(2SHORT(S)), hD(2LONG(L)), hD(3), and hD(4.4) receptors halpha(2A)-, halpha(2B)-, halpha(2C)-, halpha(1A)-adrenoceptors (ARs). As determined by guanosine 5'-O-(3-[(35)S]thio)triphosphate ([(35)S]GTPgammaS) binding, no ligand displayed "full" efficacy relative to dopamine (100%) all...
A series of new amino phosphonic acid derivatives vinblastine (1, VLB) has been synthesized and tested in vitro vivo for antitumor activity. The compounds were obtained from O4-deacetyl-VLB azide. All the products studied capable inhibiting tubulin polymerization vitro. most potent bore an alkyl substituent on phosphonate. In these compounds, anti-tumor activity strongly depended stereochemistry phosphonate (1S)-[1-[( O4-deacetyl-3-de(methoxycarbonyl)vincaleukoblastin-3-yl]...
Autotaxin is a type II ectonucleotide pyrophosphate phosphodiesterase enzyme. It has been recently discovered that it also lysophospholipase D activity. This enzyme probably provides most of the extracellular lysophosphatidic acid from lysophosphatidylcholine. The cloning and tissue distribution three isoforms (imaginatively called α, β, γ) human mouse are reported in this study, as well their by PCR mouse. fate α isoform was studied after purification using mass spectrometry. Indeed,...
Ivabradine, a specific and use-dependent I(f) inhibitor, exerts anti-ischaemic activity purely by reducing heart rate. The aim of this work was to characterize its effect on the predominant HCN channel isoform expressed in human sino-atrial nodes (hSAN), determine kinetics channels from multicellular preparations rate-dependency action.RT-PCR analysis four isoforms carried out RNAs hSAN. Patch-clamp intracellular recordings were obtained CHO cells stably expressing hHCN4 isolated SAN,...