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Title: BCL-2 family regulation by the 20S proteasome inhibitor bortezomib.
Authors: Fennell, DA
Chacko, A
Mutti, L
First Published: 21-Feb-2008
Citation: ONCOGENE, 2008, 27 (9), pp. 1189-1197
Abstract: Bortezomib (Velcade, PS341) was licensed in 2003 as a first-in-class 20S proteasome inhibitor indicated for treatment of multiple myeloma, and is currently being evaluated clinically in a range of solid tumours. The mechanisms underlying its cancer cell toxicity are complex. A growing body of evidence suggests proteasome inhibition-dependent regulation of the BCL-2 family is a critical requirement. In particular, the stabilization of BH3-only proteins BIK, NOXA and BIM, appear to be essential for effecting BAX- and BAK-dependent cell death. These mechanisms are reviewed and the implications for favourable novel drug interactions are highlighted.
DOI Link: 10.1038/sj.onc.1210744
eISSN: 1476-5594
Type: Journal Article
Appears in Collections:Published Articles, Dept. of Cancer Studies and Molecular Medicine

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