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Journal Articles Arch Pharm (Weinheim) Year : 2017

Isophthalic Acid-Based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni

Katharina Stenzel
  • Function : Author
Alokta Chakrabarti
  • Function : Author
Jelena Melesina
  • Function : Author
Finn Hansen
  • Function : Author
Julien Lancelot
Simon Herkenhohner
  • Function : Author
Beate Lungerich
  • Function : Author
Raymond Pierce
Wolfgang Sippl
Manfred Jung
  • Function : Author
T Kurz
  • Function : Author

Abstract

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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hal-03691172 , version 1 (08-06-2022)

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Katharina Stenzel, Alokta Chakrabarti, Jelena Melesina, Finn Hansen, Julien Lancelot, et al.. Isophthalic Acid-Based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni. Arch Pharm (Weinheim), 2017, 350 (8), ⟨10.1002/ardp.201700096⟩. ⟨hal-03691172⟩
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