Toward an HDAC6 inhibitor: synthesis and conformational analysis of cyclic hexapeptide hydroxamic acid designed from alpha-tubulin sequence.

@article{Jose2004TowardAH,
  title={Toward an HDAC6 inhibitor: synthesis and conformational analysis of cyclic hexapeptide hydroxamic acid designed from alpha-tubulin sequence.},
  author={Binoy Jose and Shinji Okamura and Tamaki Kato and Norikazu Nishino and Yuko Sumida and Minoru Yoshida},
  journal={Bioorganic & medicinal chemistry},
  year={2004},
  volume={12 6},
  pages={1351-6}
}
A cyclic hexapeptide hydroxamic acid inhibitor for HDAC6 has been designed and synthesized on the basis of the facts that alpha-tubulin is the substrate of HDAC6 and of the excellent inhibitory activity of cyclic tetrapeptide hydroxamic acids (CHAPs) for HDACs. Unexpectedly, cyclic hexapeptide hydroxamic acid showed very low HDAC inhibitory activity. To… CONTINUE READING