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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 34, Number 5
BKCSDE 34(5)
May 20, 2013 

 
Title
Salinosporamides A and B Inhibit Proteasome Activity and Delay the Degradation of N-end Rule Model Substrates
Author
Seung Kyun Shin, Dae in Bang, Won Hoon Choi, Seong-Hwan Kim, Dong-Chan Oh, Min Jae Lee*
Keywords
Degradation, Ubiquitin, Proteasome, Inhibitor, N-end rule
Abstract
The proteasome, which is highly evolutionarily conserved, is responsible for the degradation of most shortlived proteins in cells. Small-molecule inhibitors targeting the proteasome's degradative activity have been extensively developed as lead compounds for various human diseases. An exemplified molecule is bortezomib, which was approved by FDA in 2003 for the treatment of multiple myeloma. Here, using transiently and stably expressed N-end rule model substrates in mammalian cells, we evaluated and identified that salinosporamide A and salinosporamide B effectively inhibited the proteasomal degradation. Considering that a variety of proteasome substrates are implicated in the pathogenesis of many diseases, they have the potential to be clinically applicable as therapeutic agents.
Page
1425 - 1428
Full Text
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