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Abstract C68: SLCO1B3 influences taxane-response in prostate cancer
Conclusion: Prostate cancer cells that overexpress SLCO1B3 are more sensitive to docetaxel and cabazitaxel treatment, which could be linked to increased uptake of both taxanes. Further studies are needed to clarify the role of SLCO1B3 in the uptake of cabazitaxel into the cell. Moreover, SLCO1B3 expression affects hormonal status of prostate cancer cells as reflected by PSA production. Research is ongoing to further elucidate the role of SLCO1B3 in prostate cancer and its impact on taxane efficacy and response.Citation Format: Ellen S. de Morree, Rene Bottcher, Robert J. van Soest, Ashraf Aghai, Corrina M. de Ridder, Alice...
Source: Molecular Cancer Therapeutics - January 7, 2016 Category: Cancer & Oncology Authors: de Morree, E. S., Bottcher, R., van Soest, R. J., Aghai, A., de Ridder, C. M., Gibson, A. A., Mathijssen, R. H., Burger, H., Wiemer, E. A., Sparreboom, A., van Weerden, W. M., de Wit, R. Tags: Drug Resistance and Modifiers: Poster Presentations - Proffered Abstracts Source Type: research

Abstract A164: The small molecule UAE inhibitor TAK-243 (MLN7243) prevents DNA damage repair and reduces cell viability/tumor growth when combined with radiation, carboplatin and docetaxel
Clinical results of VELCADE® (bortezomib) For Injection have prompted evaluation of other enzymes within the ubiquitin proteasome system (UPS) as druggable targets for human cancer. We have identified a first in class investigational drug, TAK-243 (MLN7243), which targets the ubiquitin activating enzyme, UAE (UBA1), an essential cellular enzyme responsible for activating > 99% of all cellular ubiquitin. Ubiquitin is involved in multiple cellular processes including ubiquitin-dependent protein turnover, cell cycle progression, regulation of apoptosis, protein localization and response to DNA damage. Experiments combi...
Source: Molecular Cancer Therapeutics - January 7, 2016 Category: Cancer & Oncology Authors: Milhollen, M. A., Shi, J., Traore, T., Huck, J., Sappal, D., Duffy, J., Lightcap, E., Ishii, Y., Ciavarri, J., Fleming, P., Bence, N., Hyer, M. L. Tags: Therapeutic Agents: Other: Poster Presentations - Proffered Abstracts Source Type: research