Saturday November 21 2009 | Biotechnology feed | All feeds
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Saturday November 21 2009 | Biotechnology feed | All feeds
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Histone deacetylase inhibitors: An emerging class of anti-cancer drugs Basic research efforts focussing on angiogenesis as a target for cancer therapeutics have yet to bear fruit. Of the 55 molecules in development, 43 are still at preclinical stages and considerable developmental activity is expected over the next decade. Histone acetylation/deacetylation is a major factor in regulating chromatin structural dynamics during transcription. Histone deacetylase inhibitors cause hyperacetylation in chromatin usually resulting in activation of certain genes with consequent induction of terminal cell differentiation and/or apoptosis in cancer cells. Preliminary clinical studies have shown that histone hyperacetylation can be achieved safely in humans and that treatment of cancer is possible. At the beginning of last year however the therapeutic potential of histone deacetylase inhibitors was dramatically boosted by the finding that hypoxia increased the expression of this enzyme. Furthermore, a specific inhibitor of histone deacetylase, trichostatin A induced angiogenic-inhibiting factors such as von Hippel Lindau, repressed proangiogenic molecules such as hypoxia-inducible factor-1alpha and vascular endothelial growth factor and blocked the vascular endothelial growth factor signalling pathway. Related to these observations, trichostin A was a powerful blocker of angiogenesis in vitro, in vivo and in a carcinoma model. The combination of anti-angiogenic, pro-apoptitic and differentiating activity of histone deacetylase inhibitors means that they represent a class of highly exciting anti-cancer molecules. Since only a handful of novel inhibitors are reported as being in pharmaceutical development the therapeutic and commercial benefits of exploiting this pharmacological class could reach immense proportions. Histone deacetylases inhibitors as anti-angiogenic agents altering vascular endothelial growth factor signaling. Deroanne et al, Oncogene 2002 Jan 17;21(3):427-36 Interested in collaborating with this group? Contact leaddiscovery@bioportfolio.co.uk LeadDiscovery 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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