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Статті в журналах з теми "NAD – antagonistes et inhibiteurs":
Reyt, Vincent, and Jacques Buxeraud. "Hormones de croissance, agonistes, antagonistes et inhibiteurs." Actualités Pharmaceutiques 57, no. 574 (March 2018): 7–12. http://dx.doi.org/10.1016/j.actpha.2017.12.008.
Valade, Dominique. "Les avancées dans les traitements de crise et de fond de la maladie migraineuse." Biologie Aujourd'hui 213, no. 1-2 (2019): 59–64. http://dx.doi.org/10.1051/jbio/2019021.
A. EKOU. "AOD et fibrillation atriale." Les pathologies vasculaires (anciennement ANGEIOLOGIE) 71, no. 03 (September 1, 2019): 8. http://dx.doi.org/10.54695/mva.71.03.2228.
Bonnefoy, Nathalie, Daniel Olive, and Bernard Vanhove. "Les futures générations d’anticorps modulateurs des points de contrôle de la réponse immunitaire." médecine/sciences 35, no. 12 (December 2019): 966–74. http://dx.doi.org/10.1051/medsci/2019193.
Boutouyrie, Pierre, and Stéphane Laurent. "Inhibiteurs de l'enzyme de conversion et antagonistes du récepteur AT1r de l'angiotensine II." EMC - Cardiologie 1, no. 1 (January 2006): 1–9. http://dx.doi.org/10.1016/s1166-4568(01)00043-2.
Fraser, G. "Les antagonistes NK3R, nouveaux inhibiteurs de l’axe gonadotrope : mise au point et développement thérapeutique dans l’espèce humaine." Annales d'Endocrinologie 77, no. 4 (September 2016): 245. http://dx.doi.org/10.1016/j.ando.2016.07.035.
Boutouyrie, Pierre. "Inhibiteurs de l’enzyme de conversion et antagonistes calciques : une synergie d’action pour une meilleure prévention des événements cardiovasculaires." Therapies 64, no. 4 (July 2009): 241–48. http://dx.doi.org/10.2515/therapie/2009047.
Hamon, M. "Bases neurobiologiques des traitements de l’alcoolo-dépendance – Quelles perspectives ?" European Psychiatry 29, S3 (November 2014): 539. http://dx.doi.org/10.1016/j.eurpsy.2014.09.411.
Roskiewicz, France, Irina Andriamanana, Valérie Gras-Champel, Michel Andrejak, and Ziad A. Massy. "Angio-œdèmes iatrogènes: rôle des inhibiteurs de l'enzyme de conversion et des antagonistes des récepteurs à l'angiotensine II (sartans)." Néphrologie & Thérapeutique 3, no. 3 (June 2007): 89–95. http://dx.doi.org/10.1016/j.nephro.2007.03.003.
Tonnel, A. B., A. Tsicopoulos, and H. Hammad. "Les thérapeutiques du futur en allergologie. Cytokines recombinantes, anticytokines, antagonistes des récepteurs de cytokines et inhibiteurs des molécules costimulatrices." Revue Française d'Allergologie et d'Immunologie Clinique 40, no. 3 (April 2000): 295–300. http://dx.doi.org/10.1016/s0335-7457(00)80041-6.
Дисертації з теми "NAD – antagonistes et inhibiteurs":
Hasan, Bou Issa Lama. "Étude des dépendances génomiques dans le myélome multiple surexprimant MYC." Electronic Thesis or Diss., Université de Lille (2022-....), 2024. http://www.theses.fr/2024ULILS011.
Multiple myeloma (MM) is a hematological malignancy that accounts for around 13% of hematological cancers and is characterized by the uncontrolled proliferation of malignant plasma cells in the bone marrow. MM progresses from precursor stages, known as monoclonal gammopathy of undetermined significance (MGUS) and smoldering multiple myeloma (SMM), to the symptomatic form, MM. It is an incurable malignancy in which heterogeneity and clonal evolution allow treatment escape and disease progression. MYC alterations play an essential role in this progression. However, MYC is not therapeutically targetable due to its nuclear localization and the protein's short half-life.To overcome this, we hypothesized that the proliferative advantage induced by MYC overexpression creates genomic dependencies on other signalling pathways that become essential for cell survival. To test this hypothesis, we applied a novel approach by leveraging large-scale loss of function screen (Achilles) and 1869 small molecules screen to identify MYC-induced genomic vulnerabilities. When identified, these vulnerabilities offer an opportunity to selectively target cancer cells harbouring this overexpression and spare normal cells.Our analyses demonstrate the dependence of MYC overexpressing cells on glutamine metabolism, in particular on the GLS1 (glutaminase). We validated and functionally delineated this dependence in vitro using different approaches.Our small molecule screen highlighted that NAD synthesis inhibitors had a preferential effect on the proliferation of MYC overexpressing cells. Considering that glutamine and NAD have closely interlinked metabolic networks, we investigated the possibility of a potential synergistic effect between GLS1 and NAMPT inhibitors. We demonstrated the effectiveness of this new synergistic combination to target MYC-driven MM cells in vitro and in vivo.These results establish a solid methodological basis that can be used to develop new therapeutic approaches to address unmet therapeutic needs to target MYC in MM
Guilini, Pauline. "Synthèse de nouveaux inhibiteurs des fonctions plaquettaires, antagonistes des récepteurs P2Y1 et P2Y12." Strasbourg, 2011. http://www.theses.fr/2011STRA6189.
Ischemic diseases due to arterial thrombosis are the leading cause of death in developed countries. Antiplatelet agents are drugs which prevent the formation of arterial thrombosis. A therapeutic strategy consists in inhibiting the receptors responsible for platelet activation: the P2Y12 and P2Y1 receptor. For an optimal response of platelet aggregation, synergistic activation of both receptors has been demonstrated. The work described in this thesis deals with the synthesis of bivalent ligands, i. E the development of a single chemical entity that combines two antagonists targeting these receptors. This strategy may be conjugating an effective antiplatelet effect along with a sufficient hemostatic capacity. A serie of analogues of cangrelor, which are thioalkylated at C-2 position, were synthesized from 2-halogenonucleosides. The platelet aggregation tests on those compounds revealed an inhibitory effect on aggregation induced by ADP, but only in high concentrations. The preparation of a precursor of MRS2279 (a selective P2Y1 antagonist), allowed us to focus on the synthesis of heterodimers which may inhibit both receptors P2Y1 and P2Y12. Toward this goal, we combined three parts: an adenosine for the Western part, a linker (cystamine, di-, tri-and tetraethylene glycol) and a precursor of MRS2279 for the Eastern part. We performed the synthesis of several original bivalent ligands which are no phosphorylated. The dimers platelet aggregation tests show that they have no sufficient inhibitory effect to continue the biological tests. However, the phosphorylation of the two pharmacophores appears a promising approach for the activity of those bivalent ligands
Kolb, Stéphanie. "Conception, synthèse et évaluation biologique d'inhibiteurs des phosphatases CDC25 à visée anti-tumorale." Paris 5, 2009. http://www.theses.fr/2009PA05S006.
The development of CDC25 phosphatase inhibitors is an interesting approach towards new anti-tumour agents. CDC25 play key roles in cell cycle regulation and are over-expressed in numerous cancers. In order to identify promising inhibitors, we conducted in silico/in vitro screening which led to the discovery of potent molecules. [Ijpyrindine derivatives provided antiproliferative activities against cancerous cell lines but none towards a normal cell type. Structural modifications on the thiazolopyrimidine core, led to compounds which inhibit CDC25 activity and display cytotoxic activities against tumor cells. The most efficient inhibitor targets CDC25B in cells. To improve the activity of this series, novel derivatives were rapidly identified, following parallel "click" synthesis in solution and in situ screening for CDC25 inhibition. Finally, a series of dimers was designed from the thiazolopyrimidine core and evaluated for their inhibitory activity against a panel of phosphatases
Munkonda, Mercedes Nancy. "Caractérisation d'inhibiteurs des nucléoside triphosphate diphosphohydrolase-1,2,3 et 8 chez l'humain et la souris." Master's thesis, Université Laval, 2008. http://hdl.handle.net/20.500.11794/20692.
Henrion, Daniel. "Développement d'un modèle de surcharge cardio-vasculaire de calcium : réactivité vasculaire et effets des inhibiteurs de l'enzyme de conversion de l'angiotensine I et des inhibiteurs de flux calciques." Nancy 1, 1991. http://docnum.univ-lorraine.fr/public/SCD_T_1991_0454_HENRION.pdf.
Cano, Virginie. "Conception et synthèse d'inhibiteurs pour l'étude du site actif d'une UDP-glucuronosyltransférase recombinante hépatique humaine : l'UGT1*6." Nancy 1, 1997. http://www.theses.fr/1997NAN12155.
New UDP-glucuronosyltransferases inhibitors have been designed, synthetized and tested in order to probe the active sites of these proteins which are involved in the metabolism of xenobiotics, such as drugs, and endobiotics such as bilirubin, retinois acids,. . . The synthetized molecules, whose stucture is analogous to the donor substrate UDP-glucuronic acid, allowed us to characterize more specifically the peptidic domain interacting with this substrate. The maiIÏ results are gathered in three different parts, according to the group of inhibitors considered. 1- Uridine being the mother compound, a chemical series of about fifty molecules has been synthetized by varying the nature of the chemical groups placed successively on the base moiety or on the 2', 3' and 5' positions of the sugar. The inhibitory effect has frrst been estimated in terms of IC50. For the most powerful inhibitors, a detailed kinetic study gave us the inhibition constant and the type of inhibition. 2- These inhibitors have been compared to those previously obtained in the laboratory, such as arylalkyl carboxylic acids (competitive inhibitors) and N-acyl-phenylamino alcohols attached to a uridine molecule by a spacer (transition-state analogs). They have been used to characterize binding site of 4-methylumbelliferone of the UDP-glucuronosyl transferase 1. 6 after mutation of amino-acids His54 and Arg52 (mutants H54A, H54Q and R52A). 3- A series of inhibitors derived from triphenylalkyl carboxylic acids containing a primary alcohol group instead of the carboxylic acid group and with various carbon chain length has been tested on rats hepatic microsomes. They show a strong inhibitory effect on bilirubin glucuronidation. The results obtained allowed us to better understand the molecular and electronic basis of substrates interaction with UDP-glucuronosyl transferases
Scoliège-Harcouet, Laura. "Transport intestinal de bêta-lactamines orales : caractérisation et modulation par les antagonistes des canaux calciques et les inhibiteurs." Paris 11, 1995. http://www.theses.fr/1995PA114808.
Chillon, Jean-Marc. "Impact hémodynamique du vieillissement et de la surcharge calcique vasculaire chez le rat : effet des inhibiteurs de flux calciques et des inhibiteurs de l'enzyme de conversion de l'angiotensine I." Nancy 1, 1991. http://www.theses.fr/1991NAN10452.
Akue-Gedu, Rufine. "Conception rationnelle et synthèse d'inhibiteurs potentiels de la topoisomérase II : synthèse complète de la camptothécine." Lille 2, 2004. http://www.theses.fr/2004LIL2S013.
Topoisomerases I and II are target anticancer agents. Ellipticine and its derivates are good models for inhibitors of topoisomerase II. They also directly interact with DNA by intercalation. The 2-N-methyl-9-méthoxyelliptinium acetate (CEPTIUM*) was introduced in clinical treatment of breast cancer. To date it is no more commercialized because of its high toxicity. Our work was to design and to synthesize novel analogues of ellipticine obtained by modification of its structure by pharmacomodulation. Furthermore, anoriginal and full synthesis of inhibitor of topoisomerase I, the camptothecin is described. Most of the synthesized molecules have been sent for biological testings
Li, Aixiao. "Molecular modeling of non-bonding interactions in biomolecules-ligand systems." Paris 7, 2009. http://www.theses.fr/2009PA077032.
This work is devoted to modelling the interactions between some inhibitors and molecules involved in cancer development and aims at precisely establishing the interactions modes between the ligands and the biomolecules. In the CDK (cyclin dependant kinases) family we have examined the selectivity of a new inhibitor (2PU) towards CDK4 as compared to CDK2. The techniques we have used : molecular dynamics interaction energies calculation, molecular docking and mixed methods of the ONIOM type allowed us to establish the precise causes of this selectivity, showing the existence of specific interactions (H bonds, among others) between the inhibitor and CDK4. From a methodological point of view, the ONIOM method (with 2 or 3 layers) has been carefully examined with respect to the System partitioning procedure. A new approach is proposed. The stabilisation of G-quadruplex DNA by a new ligand (TQMP) has also been studied with molecular dynamics, which allowed establishing the interaction modes and show the selectivity of one of the 2 possible interaction sites
Книги з теми "NAD – antagonistes et inhibiteurs":
G, Cory Joseph, and Cory Ann H, eds. Inhibitors of ribonucleoside diphosphate reductase activity. New York: Pergamon Press, 1989.
Martin, Sarter, Nutt David J. 1951-, and Lister Richard G, eds. Benzodiazepine receptor inverse agonists. New York: Wiley-Liss, 1995.
Sitruk-Ware/Mis. Progestins and Antiprogestins in Clinical Practice. Informa Healthcare, 1999.
Mukherjee, Anil B. Biochemistry, Molecular Biology, and Physiology of Phospholipase A2 and Its Regulatory Factors. Springer, 1991.
The endothelium in cardiovascular disease: Pathophysiology, clinical presentation, and pharmacotherapy. Berlin: Springer, 1995.
Luscher, Thomas F. The Endothelium in Cardiovascular Disease: Pathophysiology, Clinical Presentation and Pharmacotherapy. Springer-Verlag Telos, 1995.
Lüscher, Thomas F. Endothelium in Cardiovascular Disease: Pathophysiology, Clinical Presentation and Pharmacotherapy. Springer London, Limited, 2011.
Luscher, Thomas F. The Endothelium in Cardiovascular Disease: Pathophysiology, Clinical Presentation, and Pharmacology. Springer-Verlag, 1995.