@article{ddf1fa7eef404f9d9f1b1f3cf937d840,
title = "Syringolin A selectively labels the 20S proteasome in murine EL4 and wild-type and bortezomib-adapted leukaemic cell lines",
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 20S 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.",
keywords = "Antitumor agents, Leukemia, Natural products, Proteasome inhibitors, Syrbactin",
author = "J{\'e}r{\^o}me Clerc and Florea, {Bogdan I.} and Marianne Kraus and Michael Groll and Robert Huber and Bachmann, {Andr{\'e} S.} and Robert Dudler and Christoph Driessen and Overkleeft, {Herman S.} and Markus Kaiser",
note = "Funding Information: Filipe S. Oliveira gratefully acknowledges the financial support of FCT/MCTES (Portugal) through the PhD fellowship SFRH/BD/73761/2010 and Isabel M. Marrucho for a contract under FCT Investigator 2012 Program. The authors also acknowledge the Funda??o para a Ci?ncia e Tecnologia (FCT) for the financial support through the project PTDC/EQUFTT/1686/2012 and Research Unit GREEN-it {"}Bioresources for Sustainability{"} (UID/Multi/04551/2013). The NMR spectrometers are part of the National NMR Facility (RECI/BBB-BQB/0230/2012), also supported by FCT.",
year = "2009",
month = nov,
day = "2",
doi = "10.1002/cbic.200900411",
language = "English",
volume = "10",
pages = "2638--2643",
journal = "ChemBioChem",
issn = "1439-4227",
publisher = "Wiley-VCH Verlag",
number = "16",
}