Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy.

  title={Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy.},
  author={Lawrence R Dick and Paul E Fleming},
  journal={Drug discovery today},
  volume={15 5-6},
Inhibition of the proteasome (a highly abundant enzymatic complex responsible for intracellular protein turnover) is an effective anti-cancer therapeutic approach, as demonstrated by the first-in-class agent bortezomib. Various new proteasome inhibitors are now in development, including peptide boronic acid analogs MLN9708 and CEP-18770, peptide epoxyketones carfilzomib and PR-047, and NPI-0052, a beta-lactone compound. All are potent inhibitors of proteasome activity in vitro but show… CONTINUE READING


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