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<publisher>HAL CCSD</publisher>
<title lang=en>A Novel Covalent mTOR Inhibitor, DHM25, Shows in Vivo Antitumor Activity against Triple-Negative Breast Cancer Cells</title>
<creator>Fouque, Amelie</creator>
<creator>Delalande, Olivier</creator>
<creator>Jean, Mickael</creator>
<creator>Castellano, Remy</creator>
<creator>Josselin, Emmanuelle</creator>
<creator>Malleter, Marine</creator>
<creator>Shoji, Kenji F.</creator>
<creator>Hung, Mac Dinh</creator>
<creator>Rampanarivo, Hariniaina</creator>
<creator>Collette, Yves</creator>
<creator>Van De Weghe, Pierre</creator>
<creator>Legembre, Patrick</creator>
<contributor>Institut de recherche, santé, environnement et travail [Rennes] (Irset) ; Université d'Angers (UA) - Université des Antilles et de la Guyane (UAG) - Université de Rennes 1 (UR1) - École des Hautes Études en Santé Publique [EHESP] (EHESP) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Institut de Génétique et Développement de Rennes (IGDR) ; Université de Rennes 1 (UR1) - Centre National de la Recherche Scientifique (CNRS) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Institut des Sciences Chimiques de Rennes (ISCR) ; Université de Rennes 1 (UR1) - Ecole Nationale Supérieure de Chimie de Rennes - Institut National des Sciences Appliquées (INSA) - Centre National de la Recherche Scientifique (CNRS)</contributor>
<contributor>Centre de Recherche en Cancérologie de Marseille (CRCM) ; Aix Marseille Université (AMU) - Institut Paoli-Calmettes - Institut National de la Santé et de la Recherche Médicale (INSERM) - Centre National de la Recherche Scientifique (CNRS)</contributor>
<contributor>Centre d'Immunologie de Marseille - Luminy (CIML) ; Aix Marseille Université (AMU) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Centre National de la Recherche Scientifique (CNRS)</contributor>
<contributor>Signalisation et Réponses aux Agents Infectieux et Chimiques (SeRAIC) ; Université de Rennes 1 (UR1) - IFR140</contributor>
<contributor>Oncogenesis Stress Signaling (OSS) ; Université de Rennes 1 (UR1) - CRLCC Eugène Marquis (CRLCC)</contributor>
<description>International audience</description>
<source>ISSN: 0022-2623</source>
<source>EISSN: 1520-4804</source>
<source>Journal of Medicinal Chemistry</source>
<publisher>American Chemical Society</publisher>
<identifier>hal-01187307</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01187307</identifier>
<source>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01187307</source>
<source>Journal of Medicinal Chemistry, American Chemical Society, 2015, 58 (16), pp.6559-6573. 〈10.1021/acs.jmedchem.5b00991〉</source>
<identifier>DOI : 10.1021/acs.jmedchem.5b00991</identifier>
<relation>info:eu-repo/semantics/altIdentifier/doi/10.1021/acs.jmedchem.5b00991</relation>
<identifier>PUBMED : 26237138</identifier>
<relation>info:eu-repo/semantics/altIdentifier/pmid/26237138</relation>
<language>en</language>
<subject>[SDV] Life Sciences [q-bio]</subject>
<type>info:eu-repo/semantics/article</type>
<type>Journal articles</type>
<description lang=en>Constitutive activation of the PI3K/mTOR signaling pathway contributes to carcinogenesis and metastasis in most, if not all, breast cancers. From a chromene backbone reported to inhibit class I PI3K catalytic subunits, several rounds of chemical syntheses led to the generation of a new collection of chromologues that showed enhanced ability to kill PI3K-addicted cancer cells and to inhibit Akt phosphorylation at serine 473, a hallmark of PI3K/mTOR activation. This initial screen uncovered a chromene designated DHM25 that exerted potent antitumor activity against breast tumor cell lines. Strikingly, DHM25 was shown to be a selective and covalent inhibitor of mTOR using biochemical and cellular analyses, modeling, and a large panel of kinase activity assays spanning the human kinome (243 kinases). Finally, in vivo, this novel drug was an efficient inhibitor of growth and metastasis of triple-negative breast cancer cells, paving the way for its clinical application in oncology</description>
<date>2015</date>
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