Syringolin A Selectively Labels the 20 S Proteasome in Murine EL4 and Wild‐Type and Bortezomib‐Adapted Leukaemic Cell Lines
作者： Jérôme Clerc , Bogdan I. Florea , Marianne Kraus , Michael Groll , Robert Huber
关键词: Molecular medicine 、 Proteasome 、 Bortezomib 、 Biochemistry 、 Wild type 、 Biology 、 Natural product 、 Small molecule 、 Cell culture 、 Proteasome inhibitor
摘要: The natural product syringolin A (SylA) is a potent proteasome inhibitor with promising anticancer activities. To further investigate its potential as lead structure, selectivity profiling cell lysates was performed. At therapeutic concentrations, rhodamine-tagged SylA derivative selectively bound to the 20 S active sites without detectable off-target labelling. Additional of wild-type and bortezomib-adapted leukaemic lines demonstrated retention this target subsite well potency even in clinically relevant lines. Our studies, therefore, propose that development might indeed result an improved small molecule for treatment leukaemia.
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Matthew Bogyo, Screening for selective small molecule inhibitors of the proteasome using activity-based probes. Methods in Enzymology. ,vol. 399, pp. 609- 622 ,(2005) , 10.1016/S0076-6879(05)99040-X
Jun Kohno, Yutaka Koguchi, Maki Nishio, Kazuya Nakao, Masataka Kuroda, Ryo Shimizu, Tetsuo Ohnuki, Saburo Komatsubara, Structures of TMC-95A-D: novel proteasome inhibitors from Apiospora montagnei sacc. TC 1093. Journal of Organic Chemistry. ,vol. 65, pp. 990- 995 ,(2000) , 10.1021/JO991375+
Martijn Verdoes, Bogdan I. Florea, Victoria Menendez-Benito, Christa J. Maynard, Martin D. Witte, Wouter A. van der Linden, Adrianus M.C.H. van den Nieuwendijk, Tanja Hofmann, Celia R. Berkers, Fijs W.B. van Leeuwen, Tom A. Groothuis, Michiel A. Leeuwenburgh, Huib Ovaa, Jacques J. Neefjes, Dmitri V. Filippov, Gijs A. van der Marel, Nico P. Dantuma, Herman S. Overkleeft, A Fluorescent Broad-Spectrum Proteasome Inhibitor for Labeling Proteasomes In Vitro and In Vivo Chemistry & Biology. ,vol. 13, pp. 1217- 1226 ,(2006) , 10.1016/J.CHEMBIOL.2006.09.013
Markus Kaiser, Michael Groll, Christian Renner, Robert Huber, Luis Moroder, Das Grundgerüst von TMC-95A als mögliche Leitstruktur für reversible Proteasominhibitoren Angewandte Chemie. ,vol. 114, pp. 817- 820 ,(2002) , 10.1002/1521-3757(20020301)114:5<817::AID-ANGE817>3.0.CO;2-7
Cord Naujokat, Dominik Fuchs, Carsten Berges, Adaptive modification and flexibility of the proteasome system in response to proteasome inhibition Biochimica et Biophysica Acta (BBA) - Molecular Cell Research. ,vol. 1773, pp. 1389- 1397 ,(2007) , 10.1016/J.BBAMCR.2007.05.007
Michael Groll, Lars Ditzel, Jan Löwe, Daniela Stock, Matthias Bochtler, Hans D. Bartunik, Robert Huber, Structure of 20S proteasome from yeast at 2.4 A resolution. Nature. ,vol. 386, pp. 463- 471 ,(1997) , 10.1038/386463A0
Jan Sterz, Ivana von Metzler, Jens-Claus Hahne, Britta Lamottke, Jessica Rademacher, Ulrike Heider, Evangelos Terpos, Orhan Sezer, The potential of proteasome inhibitors in cancer therapy Expert Opinion on Investigational Drugs. ,vol. 17, pp. 879- 895 ,(2008) , 10.1517/13543784.17.6.879
Ruud Oerlemans, Niels E. Franke, Yehuda G. Assaraf, Jacqueline Cloos, Ina van Zantwijk, Celia R. Berkers, George L. Scheffer, Kabir Debipersad, Katharina Vojtekova, Clara Lemos, Joost W. van der Heijden, Bauke Ylstra, Godefridus J. Peters, Gertjan L. Kaspers, Ben A. C. Dijkmans, Rik J. Scheper, Gerrit Jansen, Molecular basis of bortezomib resistance: proteasome subunit beta5 (PSMB5) gene mutation and overexpression of PSMB5 protein Blood. ,vol. 112, pp. 2489- 2499 ,(2008) , 10.1182/BLOOD-2007-08-104950
Matthew Bogyo, Marko Fonović, Activity-based probes as a tool for functional proteomic analysis of proteases. Expert Review of Proteomics. ,vol. 5, pp. 721- 730 ,(2008) , 10.1586/14789450.5.5.721
T Rückrich, M Kraus, J Gogel, A Beck, H Ovaa, M Verdoes, H S Overkleeft, H Kalbacher, C Driessen, Characterization of the ubiquitin-proteasome system in bortezomib-adapted cells. Leukemia. ,vol. 23, pp. 1098- 1105 ,(2009) , 10.1038/LEU.2009.8