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Prostate cancer specific derivatives of thapsigargin Cancer of the prostate forms the 2nd most common class of cancer in males in the Western world and accounts for 40,000 deaths per year in the US. Given the slow rate of proliferation of prostate cancer cells, the identification of apoptotic drugs remains one of the highest priorities for the treatment of prostate cancer. Despite considerable efforts few apoptotic candidates have progressed through to advanced stages of development. One particularly exciting target for apoptosis is the calcium signaling pathway, in particular store-operated calcium channels (SOCs) which are responsible for maintaining calcium levels in intracellular organelles. Restricted prostatic expression of the novel SOCs-related protein CaT1 has been demonstrated and linked to tumor progression. Strong evidence exist to suggest that inhibitors of CaT1 may induce apoptosis in a wide range of prostate cancer phenotypes; reduce the development of androgen-independence; and have activity in androgen-resistant cells (Click here for an overview of this target). Although blocking SOCs offers one approach to depleting intracellular calcium, this end-point can also be achieved through the use of thapsigargin and its derivatives which target intracellular stores directly to induce apoptosis in prostate cancer cells. Thapsigargin is not however selective to the prostate and to avoid the risk of side-effects, Danish researchers in collaboration with Johns Hopkins Oncology Center have developed a series of inactive Thapsigargin prodrugs that can be activated by PSA. The prodrugs thus synthesized demonstrated prostate cancer specificity suggesting that they may represent novel therapeutic candidates for this disease. Projects such as these are overviewed in full DiscoveryDossiers. DiscoveryDossiers ~ TherapeuticsAdvances ~ PharmaceuticalSolutions ~ LeadDiscovery ~ Purchase DiscoveryDossiersLeadDiscovery and BioPortfolio aims to provide reliable, insightful analysis on the biotechnology industry. However, this information is provided "as is" and no representations or warranties either express or implied of completeness, accuracy, or of any other nature are made with respect to this information. This information is neither an offer to sell nor a solicitation to buy the securities of any company. This information contains forward-looking statements, which involve risks and uncertainties which may not be listed. The biotechnology industry is an emerging industry and the securities of the companies mentioned in this report have a very high degree of risk and volatility. For this reason, this information is supplied on the condition that the reader will make his or her own determination as to its suitability for any purpose prior to any use of this information. The employees and officers of LeadDiscovery and BioPortfolio may hold positions in some or all of the stocks discussed in this report. This abstract has been produced by LeadDiscovery Ltd. Founded by life scientists for life scientists we aim to help industry identify cutting edge drug discovery options and academic/biotech institutions maximize the potential of their research. Abstracts strictly reflect the opinion of LeadDiscovery's editorial panel. While all reasonable efforts are made to ensure the accuracy of information provided LeadDiscovery and the publisher BioPortfolio, takes no responsibility for incorrect or misleading information. LeadDiscovery is designed for educational and drug development purposes only and is not intended or designed to offer medical advice or advice of any sort, and must not be used for such purpose. The information provided through LeadDiscovery and BioPortfolio should not be used for diagnosing or treating a health problem or a disease and no reliance should be placed on any information contained in this abstract or elsewhere on LeadDiscovery's and BioPortfolio's website. It is not intended to be a substitute for professional care. If you have or suspect you may have a health problem, you should consult your physician or other health care provider. |
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