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OmniScriptum Conception et synthèse d'inhibiteurs de la protéine kinase CK2: Thèse de Doctorat de l''Université Paris Descartes réalisée à l''Institut Curie ... UMR176 et INSERM U759 (Omn.Univ.Europ.)

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Description

CK2 est une protéine kinase ubiquitaire qui joue un rôle déterminant dans la survie cellulaire et exerce une puissante activité de suppression de l'apoptose. Des petites molécules inhibitrices de CK2 fourniraient à la biologie des outils pour étudier le rôle de cette kinase et permettraient d'explorer une nouvelle voie thérapeutique. Dans le but de trouver de nouveaux inhibiteurs de CK2, la Chimiothèque de l'Institut Curie a été criblée et deux familles de composés ont été mises en évidence. L'objectif de ce travail est d'améliorer les propriétés de ces molécules. D'une part, la synthèse d'analogues a permis de découvrir de nouveaux inhibiteurs puissants. D'autre part, pour mieux comprendre le mécanisme d'action de ces produits, un protocole de docking utilisant les logiciels FlexX, Gold et DOCK et le programme de simulation moléculaire CHARMM a été mis au point. Le mode de liaison à CK2 des composés actifs et les pharmacophores responsables de leur activité ont ainsi été déterminés. Ces informations constituent un point de départ pour la conception de nouveaux composés.

Product Specifications

Format
paperback
Domain
Amazon UK
Release Date
10 August 2010
Listed Since
12 August 2010

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