Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide alpha',beta'-epoxyketones.

@article{Elofsson1999TowardsSP,
  title={Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide alpha',beta'-epoxyketones.},
  author={Mikael Elofsson and Ute Splittgerber and Jayhyuk Myung and Royce Mohan and Craig M Crews},
  journal={Chemistry & biology},
  year={1999},
  volume={6 11},
  pages={811-22}
}
BACKGROUND The proteasome is a large multicatalytic protease complex (700 kDa) involved in a number of highly regulated processes. It has three major catalytic activities: a chymotrypsin-like activity, a trypsin-like activity and a post-glutamyl peptide hydrolyzing (PGPH) activity. To be useful as molecular probes, which could help dissect the cellular functions of the proteasome, inhibitors should be specific for the proteasome, active in vivo and selectively block only one of the three… CONTINUE READING

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