Probing the proteasome cavity in three steps: bio-orthogonal photo-reactive suicide substrates

Publication Type:

Journal Article

Authors:

Geurink, P.P.; Florea, B. I; Van der Marel, G.A.; Kessler, B.M.; Overkleeft, H.S.

Source:

Chemical Communications, Volume 46, p.9052-9054 (2010)

ISBN:

1364-548X (Electronic)13

DOI Name (links to online publication)

10.1039/c0cc03322g

Abstract:

Tri-functional activity-based protein probes that encompass an electrophilic trap, a photo-reactive group and a bio-orthogonal ligation handle are described. With these, and in a three-step chemical proteomics approach, proteasomal catalytic sites are covalently and irreversibly modified, followed by photocrosslinking of these to flanking subunits and Staudinger-Bertozzi ligation for visualization and identification of the resulting conjugates.