Proteasome inhibitors in cancer therapy
TLDR
This review summarises the main mechanisms of action of proteasome inhibitors in cancer, the development of prote asome inhibitors as therapeutic agents and the properties and progress of next generation proteasom inhibitors in the clinic.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.read more
Citations
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Journal Article
Proteasome Inhibitors: A Novel Class of Potent and Effective Antitumor Agents
Julian Adams,Vito J. Palombella,Edward A. Sausville,Jill R. Johnson,Antonia T. Destree,Douglas Lazarus,Jochen Maas,Christine S. Pien,Samuel Prakash,Peter J. Elliott +9 more
TL;DR: The data show that inhibition of this target site by PS-341 results in reduced tumor growth in murine tumor models and highlight that the proteasome is a novel biochemical target and that inhibitors such asPS-341 represent a unique class of antitumor agents.
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