Auswahl der wissenschaftlichen Literatur zum Thema „Recherche candidats-médicaments“
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Zeitschriftenartikel zum Thema "Recherche candidats-médicaments"
Shabajee, Preety, Albane Gaudeau, Céline Legros, Thierry Dorval und Jean-Philippe Stéphan. „Du criblage à haut contenu à la déconvolution de cibles“. médecine/sciences 37, Nr. 3 (März 2021): 249–57. http://dx.doi.org/10.1051/medsci/2021013.
Der volle Inhalt der QuelleBach, Stéphane, Pierre Colas und Marc Blondel. „La levure modèle et outil… aussi pour la recherche thérapeutique“. médecine/sciences 36, Nr. 5 (Mai 2020): 504–14. http://dx.doi.org/10.1051/medsci/2020077.
Der volle Inhalt der QuelleDissertationen zum Thema "Recherche candidats-médicaments"
Marino, Philippe. „Recherche de la preuve de principe de candidats médicaments peptidiques, dans le cadre des traumatismes médullaires“. Aix-Marseille 2, 2009. http://www.theses.fr/2009AIX22020.
Der volle Inhalt der QuelleThe overoll goal of this project is to develop a drug that would improve the quality of life of patients with spinal cord injury. In this context, the specific goal of this work was to demonstrate the proof of principle of three peptide drug candidates : a polysialic acid mimetic peptide and two peptides inhibitors of neuropilin receptors dimerization. These pharmacological targets were chosen because of their role in cellular interactions involved in plasticity events. Bio-efficacy of these three drug candidates were evaluated in validated murine models of spinal cord injury. The biophysical properties of the peptides that inhibit neuropilin activity were not compatible with their use in murine models. On the other hand, we showed that PR-21 fulfilled criteria for an in vivo use as it was not toxic, not immunogenic and displayed good stability in biological fluids or tissue. Delivery of PR-21 directly at the lesion site significantly decreased the time of return to continence, increased motor functions, sensorimotor control and coordination of hindlimbs with forelimbs in the lesioned animals. At the cellular level, we showed that PR-21 was able to increase serotoninergic axons density at and caudal to the lesion site, and to act on astrocytes by decreasing reactive gliosis. In an in vitro model of reactive astrocytes PR-21 modulated NCAM140 expression in strongly GFAP positive cells. Our data points to unique features and properties of a carbohydrate mimicking peptide and supports the notion that PSA-NCAM is an important factor to consider to treat spinal cord injury. In light of these results, PR-21 appears to be a promising therapeutic compound for acute CNS injuries
Delehouzé, Claire. „Approche chémobiologique d’étude de la régulation moléculaire de la mort cellulaire programmée par nécrose pour l’optimisation de nouveaux candidats médicaments“. Electronic Thesis or Diss., Sorbonne université, 2023. http://www.theses.fr/2023SORUS605.
Der volle Inhalt der QuelleThe concept of programmed cell death first appeared in the literature in the mid-1960s. In 1972, the term "apoptosis" was used to describe a major mechanism of programmed cell death, as opposed to accidental death by necrosis. Since the mid-2000s, other non-apoptotic pathways of regulated cell death have been identified; these manifest the phenotypic features of necrotic death. These pathways are classified according to the molecular regulators involved in each. Two of these pathways, known as necroptosis and ferroptosis, are being extensively studied because of their imputed roles in severe acute and chronic pathologies for which there are currently no effective treatments. Understanding the molecular mechanisms driving necroptosis and ferroptosis is crucial for the development of new targeted therapies. Indeed, identifying the molecular players involved in these cell death pathways will lead to the identification of novel pharmacological targets and subsequent screening for therapeutic drugs. Moreover, as the coactivation of these regulated necrotic pathways occurs in a number of common pathologies, the development of multi-target inhibitors (that is, a polypharmacological strategy) is a path-breaking avenue of research. Indeed, targeting two or more regulated necrosis pathways with a single molecule would be expected to be markedly more effective than targeting a single pathway. SeaBeLife Biotech, the industrial partner of this CIFRE thesis, is developing necroptosis and ferroptosis inhibitors, as well as first-in-class dual inhibitors (i.e. those that inhibit both necrotic cell death pathways simultaneously).The aims of this thesis work were (i) to study the cellular effects of necroptosis and ferroptosis inhibitors developed in a collaboration among the Roscoff Biological Station, the universities of Lyon and Rennes, and SeaBeLife Biotech; (ii) to identify the cellular targets of these molecules in order to refine our understanding of their mechanism of action; and (iii) to propose new drug candidates to be developed by SeaBeLife Biotech. Work was conducted on the study of two of SeaBeLife's pioneering molecules, belonging to distinct chemical families, and featuring dual inhibition of necroptosis and ferroptosis. Further studies focused on one molecule, the 7-azaindole derivative SBL01, which is SeaBeLife Biotech's most advanced product. SBL01 will shortly enter the regulatory pre-clinical phase of testing. SBL01 targets were investigated by reverse screening using small molecules functionally derivatized grafted onto solid matrices. These matrices were used as affinity chromatography ligands, in order to purify and identify a new SBL01 target of interest. A large-scale transcriptomic study was also used, to identify phenotypic marker genes and complete the characterization of the mechanism of action of SBL01. This work has thus led to the proposal of innovative screening assays that could lead to the emergence of new drug candidates. Therapeutic applications range from renal failure and acute liver failure (particularly in the case of drug overdose) to chronic neurodegenerative pathologies
Conan, Pierre. „Identification d'inhibiteurs de la Cystathionine-β-Synthase, une enzyme dont la surexpression est impliquée dans la déficience intellectuelle dans la trisomie 21“. Electronic Thesis or Diss., Brest, 2023. http://www.theses.fr/2023BRES0102.
Der volle Inhalt der QuelleDown syndrome is a genetic disorder resulting from an additional chromosome in the 21st pair. Patientssuffering from DS are characterized by craniofacial dysmorphia, cardiomyopathy and an increased incidence of Alzheimer’s disease. Patients also suffer from intellectual disability, with variable degrees of severity, for which there is so far no treatment. Many studies have focused on the identification of genes which triplication may be involved in the intellectual disability, in order to develop a treatment. These studies have identified two genes located on chromosome 21: DYRK1A, encoding a tyrosine kinase regulating many signaling pathways, and CBS, encoding the Cystathionine-Beta-Synthase, responsible for the sulfur amino acid metabolization and H2S production, an essential gasotransmitter for synaptic transmission. My PhD project aims at identifying pharmaceutical drug candidates able to decrease CBS enzymatic activity. I have already identified two promising families of compounds sharing the property of having a high affinity for metallic ions. Moreover, we have characterized a genetic link between DYRK1A and CBS. The Characterization of the link between these two enzymes should allow the identification of new therapeutical approaches to treat intellectual disability in Down Syndrome
Buchteile zum Thema "Recherche candidats-médicaments"
„Recherche de sondes pharmacologiques et candidats médicaments dans le cyberespace“. In Chimie et nouvelles thérapies, 147–70. EDP Sciences, 2020. http://dx.doi.org/10.1051/978-2-7598-2478-6-010.
Der volle Inhalt der Quelle„Recherche de sondes pharmacologiques et candidats médicaments dans le cyberespace“. In Chimie et nouvelles thérapies, 147–70. EDP Sciences, 2020. http://dx.doi.org/10.1051/978-2-7598-2478-6.c010.
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