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J Cell Commun Signal. 2011 Jun;5(2):101-10. doi: 10.1007/s12079-011-0121-7. Epub 2011 Jan 31.

Proteasome inhibitors in cancer therapy.

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Centre for Cancer Research and Cell Biology, Queen's University Belfast, Ground Floor, 97 Lisburn Road, Belfast, Northern Ireland, BT9 7BL.

Abstract

The ubiquitin proteasome pathway plays a critical role in regulating many processes in the cell which are important for tumour cell growth and survival. Inhibition of proteasome function has emerged as a powerful strategy for anti-cancer therapy. Clinical validation of the proteasome as a therapeutic target was achieved with bortezomib and has prompted the development of a second generation of proteasome inhibitors with improved pharmacological properties. This review summarises the main mechanisms of action of proteasome inhibitors in cancer, the development of proteasome inhibitors as therapeutic agents and the properties and progress of next generation proteasome inhibitors in the clinic.

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