title: 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.
authors.affiliation: Leiden Institute of Chemistry and Netherlands Proteomics Centre, P.O. Box 9502, 2300 RA, Leiden, The Netherlands.
authors.forename: Wouter A
authors.initials: WA
authors.lastname: van der Linden
authors.forename: Paul P
authors.initials: PP
authors.lastname: Geurink
authors.forename: Chris
authors.initials: C
authors.lastname: Oskam
authors.forename: Gijsbert A
authors.initials: GA
authors.lastname: van der Marel
authors.forename: Bogdan I
authors.initials: BI
authors.lastname: Florea
authors.forename: Herman S
authors.initials: HS
authors.lastname: Overkleeft
mesh_terms: D000818:Animals; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism*; D061988:Proteasome Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D009842:Oligopeptides; D061988:Proteasome Inhibitors; D046988:Proteasome Endopeptidase Complex