KOPS - Das Institutionelle Repositorium der Universität Konstanz

A Novel Microtubule Inhibitor 4SC-207 with Anti-Proliferative Activity in Taxane-Resistant Cells

A Novel Microtubule Inhibitor 4SC-207 with Anti-Proliferative Activity in Taxane-Resistant Cells

Zitieren

Dateien zu dieser Ressource

Prüfsumme: MD5:f27f33447e47b9b0f51022868c3d8dbc

BAUSCH, Elena, Hella KOHLHOF, Svetlana HAMM, Rolf KRAUSS, Roland BAUMGARTNER, Lucia SIRONI, 2013. A Novel Microtubule Inhibitor 4SC-207 with Anti-Proliferative Activity in Taxane-Resistant Cells. In: PLoS ONE. 8(11), e79594. eISSN 1932-6203. Available under: doi: 10.1371/journal.pone.0079594

@article{Bausch2013Novel-26342, title={A Novel Microtubule Inhibitor 4SC-207 with Anti-Proliferative Activity in Taxane-Resistant Cells}, year={2013}, doi={10.1371/journal.pone.0079594}, number={11}, volume={8}, journal={PLoS ONE}, author={Bausch, Elena and Kohlhof, Hella and Hamm, Svetlana and Krauss, Rolf and Baumgartner, Roland and Sironi, Lucia}, note={Article Number: e79594} }

Kohlhof, Hella Bausch, Elena Hamm, Svetlana A Novel Microtubule Inhibitor 4SC-207 with Anti-Proliferative Activity in Taxane-Resistant Cells Krauss, Rolf Krauss, Rolf Kohlhof, Hella Microtubule inhibitors are invaluable tools in cancer chemotherapy: taxanes and vinca alkaloids have been successfully used in the clinic over the past thirty years against a broad range of tumors. However, two factors have limited the effectiveness of microtubule inhibitors: toxicity and resistance. In particular, the latter is highly unpredictable, variable from patient to patient and is believed to be the cause of treatment failure in most cases of metastatic cancers. For these reasons, there is an increasing demand for new microtubule inhibitors that can overcome resistance mechanisms and that, at the same time, have reduced side effects. Here we present a novel microtubule inhibitor, 4SC-207, which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI<sub>50</sub> of 11nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. In summary, our results suggest that 4SC-207 may be a potential anti-cancer agent. 2013 deposit-license Baumgartner, Roland PLoS ONE ; 8 (2013), 11. - e79594 Baumgartner, Roland Sironi, Lucia Bausch, Elena 2014-02-11T14:44:23Z Hamm, Svetlana eng 2014-02-11T14:44:23Z Sironi, Lucia

Dateiabrufe seit 01.10.2014 (Informationen über die Zugriffsstatistik)

Bausch_263425.pdf 106

Das Dokument erscheint in:

KOPS Suche


Stöbern

Mein Benutzerkonto