Fiche publication


Date publication

juin 2017

Journal

Archiv der Pharmazie

Auteurs

Membres identifiés du Cancéropôle Est :
Dr ROMIER Christophe


Tous les auteurs :
Stenzel K, Chakrabarti A, Melesina J, Hansen FK, Lancelot J, Herkenhöhner S, Lungerich B, Marek M, Romier C, Pierce RJ, Sippl W, Jung M, Kurz T

Résumé

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.

Mots clés

Docking studies, HDAC8, Histone deacetylase inhibitors, Schistosoma mansoni, Schistosomiasis

Référence

Arch. Pharm. (Weinheim). 2017 Jun;: