Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.

@article{Whitehead2011HumanHI,
  title={Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.},
  author={Lewis Whitehead and Markus R Dobler and Branko Radetich and Yanyi Zhu and Peter W Atadja and Tavina Claiborne and Jonathan E Grob and Andrew J McRiner and Margaret R Pancost and Anup Patnaik and Wenlin Shao and Michael Shultz and Ritesh B. Tichkule and Ruben A Tommasi and Brian Vash and Ping Wang and Travis Stams},
  journal={Bioorganic & medicinal chemistry},
  year={2011},
  volume={19 15},
  pages={4626-34}
}
Herein we report the discovery of a family of novel yet simple, amino-acid derived class I HDAC inhibitors that demonstrate isoform selectivity via access to the internal acetate release channel. Isoform selectivity criteria is discussed on the basis of X-ray crystallography and molecular modeling of these novel inhibitors bound to HDAC8, potentially revealing insights into the mechanism of enzymatic function through novel structural features revealed at the atomic level. 

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