Structure-Based Design and Biological Characterization of Selective Histone Deacetylase 8 (HDAC8) Inhibitors with Anti-Neuroblastoma Activity.

@article{Heimburg2017StructureBasedDA,
  title={Structure-Based Design and Biological Characterization of Selective Histone Deacetylase 8 (HDAC8) Inhibitors with Anti-Neuroblastoma Activity.},
  author={Tino Heimburg and Fiona R. Kolbinger and Patrik Zeyen and Esraa Ghazy and Daniel Herp and Karin Schmidtkunz and Jelena Melesina and Tajith B Shaik and Frank Erdmann and Matthias C. Schmidt and Christophe Romier and Dina Robaa and Olaf Witt and Ina Oehme and Manfred Jung and Wolfgang Sippl},
  journal={Journal of medicinal chemistry},
  year={2017},
  volume={60 24},
  pages={
          10188-10204
        }
}
Histone deacetylases (HDACs) are important modulators of epigenetic gene regulation and additionally control the activity of non-histone protein substrates. While for HDACs 1-3 and 6 many potent selective inhibitors have been obtained, for other subtypes much less is known on selective inhibitors and the consequences of their inhibition. The present report describes the development of substituted benzhydroxamic acids as potent and selective HDAC8 inhibitors. Docking studies using available… CONTINUE READING
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