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An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.
Chaikuad, Apirat; Diharce, Julien; Schröder, Martin; Foucourt, Alicia; Leblond, Bertrand; Casagrande, Anne-Sophie; Désiré, Laurent; Bonnet, Pascal; Knapp, Stefan; Besson, Thierry.
Afiliación
  • Chaikuad A; Target Discovery Institute (TDI), and Structural Genomics Consortium (SGC), University of Oxford , Old Road Campus Research Building, Oxford OX3 7DQ, U.K.
  • Diharce J; Institut de Chimie Organique et Analytique, UMR CNRS-Université d'Orléans 7311, Université d'Orléans , BP 6759, Orléans 45067 Cedex 2, France.
  • Schröder M; Institute of Pharmaceutical Chemistry and Buchman Institute for Life Sciences, Goethe-University , Max-von-Laue-Strasse 9, 60438 Frankfurt am Main, Germany.
  • Foucourt A; Normandie Univ, UNIROUEN, INSA Rouen, CNRS , COBRA UMR 6014, 76000 Rouen, France.
  • Leblond B; Diaxonhit , 63-65 Boulevard Masséna, 75013 Paris, France.
  • Casagrande AS; Diaxonhit , 63-65 Boulevard Masséna, 75013 Paris, France.
  • Désiré L; Diaxonhit , 63-65 Boulevard Masséna, 75013 Paris, France.
  • Bonnet P; Institut de Chimie Organique et Analytique, UMR CNRS-Université d'Orléans 7311, Université d'Orléans , BP 6759, Orléans 45067 Cedex 2, France.
  • Knapp S; Target Discovery Institute (TDI), and Structural Genomics Consortium (SGC), University of Oxford , Old Road Campus Research Building, Oxford OX3 7DQ, U.K.
  • Besson T; Institute of Pharmaceutical Chemistry and Buchman Institute for Life Sciences, Goethe-University , Max-von-Laue-Strasse 9, 60438 Frankfurt am Main, Germany.
J Med Chem ; 59(22): 10315-10321, 2016 11 23.
Article en En | MEDLINE | ID: mdl-27766861
Methyl 9-anilinothiazolo[5,4-f]quinazoline-2-carbimidates 1 (EHT 5372) and 2 (EHT 1610) are strong inhibitors of DYRK's family kinases. The crystal structures of the complex revealed a noncanonical binding mode of compounds 1 and 2 in DYRK2, explaining the remarkable selectivity and potency of these inhibitors. The structural data and comparison presented here provide therefore a template for further improvement of this inhibitor class and for the development of novel inhibitors selectively targeting DYRK kinases.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinazolinas / Proteínas Tirosina Quinasas / Inhibidores de Proteínas Quinasas Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Estados Unidos
Buscar en Google
Añadir a Mi BVS
Imprimir
XML
PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinazolinas / Proteínas Tirosina Quinasas / Inhibidores de Proteínas Quinasas Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Estados Unidos