Proteasome selectivity towards Michael acceptor containing oligopeptide-based inhibitors.

Abstract

The synthesis and biological evaluation of ten Michael acceptors containing potential proteasome inhibitors are described. Cellular targets of azide containing inhibitors and were assessed in HEK293T and RAW264.7 cells by a two step labeling strategy, followed by biotin-pulldown, affinity purification, on-bead tryptic digestion and LC-MS(2) identification. This strategy appears to be an attractive alternative to gel-based competition assays.

DOI: 10.1039/b924134e

Cite this paper

@article{Linden2010ProteasomeST, title={Proteasome selectivity towards Michael acceptor containing oligopeptide-based inhibitors.}, author={Wouter A. van der Linden and Paul P. Geurink and Chris Oskam and Gijsbert A. van der Marel and Bogdan I. Florea and Herman S Overkleeft}, journal={Organic & biomolecular chemistry}, year={2010}, volume={8 8}, pages={1885-93} }