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Open AccessArticle

Effects of Sorafenib on C-Terminally Truncated Androgen Receptor Variants in Human Prostate Cancer Cells

1
Department of Urology, Ulm University, Ulm 89075, Germany
2
Department of Physiology, Charité Universitätsmedizin, Campus Benjamin Franklin, Berlin 14195, Germany
3
Institute of General Zoology and Endocrinology, Ulm University, Ulm 89069, Germany
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Int. J. Mol. Sci. 2012, 13(9), 11530-11542; https://doi.org/10.3390/ijms130911530
Received: 7 August 2012 / Revised: 5 September 2012 / Accepted: 6 September 2012 / Published: 14 September 2012
(This article belongs to the Special Issue Advances in Molecular Oncology (special issue))
Recent evidence suggests that the development of castration resistant prostate cancer (CRPCa) is commonly associated with an aberrant, ligand-independent activation of the androgen receptor (AR). A putative mechanism allowing prostate cancer (PCa) cells to grow under low levels of androgens, is the expression of constitutively active, C-terminally truncated AR lacking the AR-ligand binding domain (LBD). Due to the absence of a LBD, these receptors, termed ARΔLBD, are unable to respond to any form of anti-hormonal therapies. In this study we demonstrate that the multikinase inhibitor sorafenib inhibits AR as well as ARΔLBD-signalling in CRPCa cells. This inhibition was paralleled by proteasomal degradation of the AR- and ARΔLBD-molecules. In line with these observations, maximal antiproliferative effects of sorafenib were achieved in AR and ARΔLBD-positive PCa cells. The present findings warrant further investigations on sorafenib as an option for the treatment of advanced AR-positive PCa. View Full-Text
Keywords: sorafenib; truncated androgen receptor variants; castration resistant prostate cancer sorafenib; truncated androgen receptor variants; castration resistant prostate cancer
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Zengerling, F.; Streicher, W.; Schrader, A.J.; Schrader, M.; Nitzsche, B.; Cronauer, M.V.; Höpfner, M. Effects of Sorafenib on C-Terminally Truncated Androgen Receptor Variants in Human Prostate Cancer Cells. Int. J. Mol. Sci. 2012, 13, 11530-11542.

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