Issue 47, 2010
From the journal:

Chemical Communications

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

Paul P. Geurink,a   Bogdan I. Florea,a   Gijs A. Van der Marel,a   Benedikt M. Kessler*b  and  Herman S. Overkleeft*a  

* Corresponding authors

a Leiden Institute of Chemistry and Netherlands Proteomics Centre, Gorlaeus Laboratories, Einsteinweg 55, 2333 CC Leiden, The Netherlands
E-mail: h.s.overkleeft@chem.leidenuniv.nl
Fax: +31 71 527 4307
Tel: +31 71 527 4342

b Henry Wellcome Building for Molecular Physiology, Department of Clinical Medicine, University of Oxford, Roosevelt Drive, Oxford, UK
E-mail: bmk@ccmp.ox.ac.uk

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.

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

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Article information

DOI
https://doi.org/10.1039/C0CC03322G
Article type
Communication
Submitted
18 Aug 2010
Accepted
08 Oct 2010
First published
27 Oct 2010

Chem. Commun., 2010,46, 9052-9054

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

P. P. Geurink, B. I. Florea, G. A. Van der Marel, B. M. Kessler and H. S. Overkleeft, Chem. Commun., 2010, 46, 9052 DOI: 10.1039/C0CC03322G

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