α-Keto phenylamides as P1'-extended proteasome inhibitors.

@article{Voss2014KetoPA,
  title={α-Keto phenylamides as P1'-extended proteasome inhibitors.},
  author={Constantin Voss and Christoph Scholz and Sabine Knorr and Philipp Beck and Martin Lorenz Stein and Andrea Zall and Ulrike Kuckelkorn and Peter M Kloetzel and Michael Groll and Kay Hamacher and Boris Schmidt},
  journal={ChemMedChem},
  year={2014},
  volume={9 11},
  pages={
          2557-64
        }
}
The major challenge for proteasome inhibitor design lies in achieving high selectivity for, and activity against, the target, which requires specific interactions with the active site. Novel ligands aim to overcome off-target-related side effects such as peripheral neuropathy, which is frequently observed in cancer patients treated with the FDA-approved proteasome inhibitors bortezomib (1) or carfilzomib (2). A systematic comparison of electrophilic headgroups recently identified the class of… CONTINUE READING
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