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Syringolin A selectively labels the 20 S proteasome in murine EL4 and wild-type and bortezomib-adapted leukaemic cell lines

Clerc, Jérôme, Florea, Bogdan I., Kraus, Marianne, Groll, Michael, Huber, Robert, Bachmann, André S., Dudler, Robert, Driessen, Christoph, Overkleeft, Herman S. and Kaiser, Markus 2009. Syringolin A selectively labels the 20 S proteasome in murine EL4 and wild-type and bortezomib-adapted leukaemic cell lines. ChemBioChem 10 (16) , pp. 2638-2643. 10.1002/cbic.200900411

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Abstract

The natural product syringolin A (SylA) is a potent proteasome inhibitor with promising anticancer activities. To further investigate its potential as a lead structure, selectivity profiling with cell lysates was performed. At therapeutic concentrations, a rhodamine-tagged SylA derivative selectively bound to the 20 S proteasome active sites without detectable off-target labelling. Additional profiling with lysates of wild-type and bortezomib-adapted leukaemic cell lines demonstrated the retention of this proteasome target and subsite selectivity as well as potency even in clinically relevant cell lines. Our studies, therefore, propose that further development of SylA might indeed result in an improved small molecule for the treatment of leukaemia.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Subjects: Q Science > Q Science (General)
Uncontrolled Keywords: antitumor agents; leukemia; natural products; proteasome inhibitors; syrbactin
Publisher: John Wiley & Sons
ISSN: 1439-4227
Last Modified: 24 Jun 2017 08:42
URI: http://orca-mwe.cf.ac.uk/id/eprint/17991

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