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<publisher>HAL CCSD</publisher>
<title lang=en>Sibiriline, a new small chemical inhibitor of receptor-interacting protein kinase 1, prevents immune-dependent hepatitis</title>
<creator>Le Cann, F.</creator>
<creator>Delehouzé, C.</creator>
<creator>Leverrier-Penna, S.</creator>
<creator>Filliol, A.</creator>
<creator>Comte, A.</creator>
<creator>Delalande, O.</creator>
<creator>Desban, N.</creator>
<creator>Baratte, B.</creator>
<creator>Gallais, I.</creator>
<creator>Piquet-Pellorce, C.</creator>
<creator>Faurez, F.</creator>
<creator>Bonnet, M.</creator>
<creator>Mettey, Y.</creator>
<creator>Goekjian, P.</creator>
<creator>Samson, M.</creator>
<creator>Vandenabeele, P.</creator>
<creator>Bach, S.</creator>
<creator>Dimanche-Boitrel, M.-T.</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>Phophorylation de protéines et Pathologies Humaines (P3H) ; Université Pierre et Marie Curie - Paris 6 (UPMC) - Centre National de la Recherche Scientifique (CNRS)</contributor>
<contributor>Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS) ; Université Claude Bernard Lyon 1 (UCBL) - Institut National des Sciences Appliquées de Lyon (INSA Lyon) - École Supérieure Chimie Physique Électronique de Lyon - Centre National de la Recherche Scientifique (CNRS)</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>Faculté de Médecine et de Pharmacie - Université de Poitiers ; Université de Poitiers</contributor>
<contributor>Ghent University [Belgium] (UGENT)</contributor>
<contributor>Conseil Régional de Bretagne</contributor>
<contributor> FWO G.0787.13N, FWO, Fonds Wetenschappelijk Onderzoek</contributor>
<contributor> Ligue Contre le Cancer</contributor>
<contributor> Universiteit Gent</contributor>
<contributor> UEB, Université Européenne de Bretagne</contributor>
<contributor> VIB, Vlaams Instituut voor Biotechnologie</contributor>
<contributor> FWO G.0875.11, FWO, Fonds Wetenschappelijk Onderzoek</contributor>
<contributor> FWO G.0A45.12N, FWO, Fonds Wetenschappelijk Onderzoek</contributor>
<contributor> FWO G.0C37.14N, FWO, Fonds Wetenschappelijk Onderzoek</contributor>
<contributor> FWO G.0E04.16N, FWO, Fonds Wetenschappelijk Onderzoek</contributor>
<contributor> IAP 7/32, BELSPO, Federaal Wetenschapsbeleid</contributor>
<contributor> PLBIO2012, INCa, Institut National Du Cancer</contributor>
<description>International audience</description>
<source>ISSN: 1742464X</source>
<source>FEBS Journal</source>
<identifier>hal-01616420</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01616420</identifier>
<source>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01616420</source>
<source>FEBS Journal, 2017, 284 (18), pp.3050-3068. 〈10.1111/febs.14176〉</source>
<identifier>DOI : 10.1111/febs.14176</identifier>
<relation>info:eu-repo/semantics/altIdentifier/doi/10.1111/febs.14176</relation>
<identifier>PUBMED : 28715128</identifier>
<relation>info:eu-repo/semantics/altIdentifier/pmid/28715128</relation>
<language>en</language>
<subject lang=en>Concanavalin A -induced hepatitis</subject>
<subject lang=en>kinase inhibitor</subject>
<subject lang=en>molecular docking</subject>
<subject lang=en>necroptosis</subject>
<subject lang=en>RIPK1 inhibitor</subject>
<subject>[SDV.GEN] Life Sciences [q-bio]/Genetics</subject>
<type>info:eu-repo/semantics/article</type>
<type>Journal articles</type>
<description lang=en>Necroptosis is a regulated form of cell death involved in several disease models including in particular liver diseases. Receptor-interacting protein kinases, RIPK1 and RIPK3, are the main serine/threonine kinases driving this cell death pathway. We screened a noncommercial, kinase-focused chemical library which allowed us to identify Sibiriline as a new inhibitor of necroptosis induced by tumor necrosis factor (TNF) in Fas-associated protein with death domain (FADD)-deficient Jurkat cells. Moreover, Sib inhibits necroptotic cell death induced by various death ligands in human or mouse cells while not protecting from caspase-dependent apoptosis. By using competition binding assay and recombinant kinase assays, we demonstrated that Sib is a rather specific competitive RIPK1 inhibitor. Molecular docking analysis shows that Sib is trapped closed to human RIPK1 adenosine triphosphate-binding site in a relatively hydrophobic pocket locking RIPK1 in an inactive conformation. In agreement with its RIPK1 inhibitory property, Sib inhibits both TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis. Finally, Sib protects mice from concanavalin A-induced hepatitis. These results reveal the small-molecule Sib as a new RIPK1 inhibitor potentially of interest for the treatment of immune-dependent hepatitis. © 2017 Federation of European Biochemical Societies</description>
<date>2017</date>
</dc>
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