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Isophthalic Acid-Based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni.
Stenzel, Katharina; Chakrabarti, Alokta; Melesina, Jelena; Hansen, Finn K; Lancelot, Julien; Herkenhöhner, Simon; Lungerich, Beate; Marek, Martin; Romier, Christophe; Pierce, Raymond J; Sippl, Wolfgang; Jung, Manfred; Kurz, Thomas.
Afiliación
  • Stenzel K; Institute of Pharmaceutical and Medicinal Chemistry, Heinrich-Heine-University, Düsseldorf, Germany.
  • Chakrabarti A; Institute of Pharmaceutical Sciences, Albert-Ludwigs-University Freiburg, Freiburg, Germany.
  • Melesina J; Institute of Pharmacy, Martin-Luther-University Halle-Wittenberg, Halle (Saale), Germany.
  • Hansen FK; Institute of Pharmaceutical and Medicinal Chemistry, Heinrich-Heine-University, Düsseldorf, Germany.
  • Lancelot J; Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Leipzig University, Leipzig, Germany.
  • Herkenhöhner S; Univ. Lille, CNRS, Inserm, CHU Lille, Institut Pasteur de Lille, U1019 UMR 8204CIIL - Centre d'Infection et d'Immunité de Lille, Lille, France.
  • Lungerich B; Institute of Pharmaceutical and Medicinal Chemistry, Heinrich-Heine-University, Düsseldorf, Germany.
  • Marek M; Institute of Pharmaceutical and Medicinal Chemistry, Heinrich-Heine-University, Düsseldorf, Germany.
  • Romier C; IGBMC, Université de Strasbourg, Illkirch, France.
  • Pierce RJ; IGBMC, Université de Strasbourg, Illkirch, France.
  • Sippl W; Univ. Lille, CNRS, Inserm, CHU Lille, Institut Pasteur de Lille, U1019 UMR 8204CIIL - Centre d'Infection et d'Immunité de Lille, Lille, France.
  • Jung M; Institute of Pharmacy, Martin-Luther-University Halle-Wittenberg, Halle (Saale), Germany.
  • Kurz T; Institute of Pharmaceutical Sciences, Albert-Ludwigs-University Freiburg, Freiburg, Germany.
Arch Pharm (Weinheim) ; 350(8)2017 Aug.
Article en En | MEDLINE | ID: mdl-28639720
Schistosoma mansoni histone deacetylase 8 (SmHDAC8) has been recently identified as a new potential target for the treatment of schistosomiasis. A series of newly designed and synthesized alkoxyamide-based and hydrazide-based HDAC inhibitors were tested for inhibitory activity against SmHDAC8 and human HDACs 1, 6, and 8. The front runner compounds showed submicromolar activity against SmHDAC8 and modest preference for SmHDAC8 over its human orthologue hHDAC8. Docking studies provided insights into the putative binding mode in SmHDAC8 and allowed rationalization of the observed selectivity profile.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ácidos Ftálicos / Proteínas Represoras / Esquistosomicidas / Inhibidores de Histona Desacetilasas Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: Arch Pharm (Weinheim) Año: 2017 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Alemania
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ácidos Ftálicos / Proteínas Represoras / Esquistosomicidas / Inhibidores de Histona Desacetilasas Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: Arch Pharm (Weinheim) Año: 2017 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Alemania