Journal
FEBS LETTERS
Volume 581, Issue 25, Pages 4955-4959Publisher
WILEY
DOI: 10.1016/j.febslet.2007.09.031
Keywords
betulinic acid; proteasome inhibitor; proteasome activator
Funding
- NIAID NIH HHS [R01 AI065310, R01 AI052022-05, AI52022, AI65310, R01 AI065310-02, R01 AI052022] Funding Source: Medline
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This study discovered that betulinic acid (BA) is a potent proteasome activator that preferentially activates the chymotrypsin-like activity of the proteasome. Chemical modifications can transform BA into proteasome inhibitors. Chemical modifications at the C-3 position of BA resulted in compounds, such as dimethylsuccinyl BA (DSB), with various inhibitory activities against the human 20S proteasome. Interestingly, the proteasomal activation by BA and the inhibitory activity of DSB could be abrogated by introducing a side chain at the C-28 position. In summary, this study discovered a class of small molecules that can either activate or inhibit human proteasome activity depending on side chain modifications. (c) 2007 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
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