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

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Inhibition of the proteasome 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. In this review the authors review the second-generation proteasome inhibitors and assess the potential pharmacologic impact of their different chemical properties.

The concept of proteasome inhibition as a therapeutic approach in cancer is now well established, and numerous companies are now developing new proteasome inhibitors with the aim of building upon the success of the first-in-class inhibitor bortezomib.

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