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Paper

Org. Biomol. Chem., 2007, 5, 1416 - 1426, DOI: 10.1039/b702268a

Mixing of peptides and electrophilic traps gives rise to potent, broad-spectrum proteasome inhibitors

Martijn Verdoes, Bogdan I. Florea, Wouter A. van der Linden, Didier Renou, Adrianus M. C. H. van den Nieuwendijk, Gijs A. van der Marel and Herman S. Overkleeft

The synthesis and evaluation of hybrid proteasome inhibitors that contain structural elements of the known inhibitors bortezomib, epoxomicin and peptide vinyl sulfones is described. From the panel of 15 inhibitors some structure activity relationships can be deduced with regard to inhibitory activity in relation to peptide recognition element, inhibitor size and nature of the electrophilic trap. Further, the panel contains one of the most potent peptide-based pan-proteasome inhibitors reported to date.

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