Subtype selective substrates for histone deacetylases.

@article{Heltweg2004SubtypeSS,
  title={Subtype selective substrates for histone deacetylases.},
  author={Birgit Heltweg and Franck Dequiedt and Brett L Marshall and Carsten Brauch and Minoru Yoshida and Norikazu Nishino and Eric Verdin and Manfred Jung},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 21},
  pages={
          5235-43
        }
}
  • Birgit Heltweg, Franck Dequiedt, +5 authors Manfred Jung
  • Published in
    Journal of medicinal…
    2004
  • Chemistry, Medicine
  • To probe the steric requirements for deacylation, we synthesized lysine-derived small molecule substrates and examined structure-reactivity relationships with various histone deacetylases. Rat liver, human HeLa, and human recombinant class I and II histone deacetylases (HDACs) as well as human recombinant NAD(+)-dependent SIRT1 (class III enzyme) were used in these studies. A benzyloxycarbonyl substituent on the alpha-amino group yielded the highest conversion rates. Replacing the epsilon… CONTINUE READING

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