Design of selective inhibitors for human immunoproteasomes

Abstract

The thesis describes the development, synthesis and biological evaluation of several proteasome inhibitor designs. Mainly, this work focusses on designing proteasome inhibitors that selectively inhibit the immunoproteasome, while leaving the constitutive proteasome mostly, if not completely, untouched.

20S proteasomeEpoxyketoneProteasome inhibitorElectrophilic trapMultiple MyelomaEpoxomicinAcitivity-based protein profiling