Abstract
The proteasome continues to be an attractive target for cancer drug discovery and was validated as such by the successful development of bortezomib. Despite its remarkable efficacy, concerns regarding side effects and drug resistance limit the widespread application of bortezomib. Thus, there has been a heightened interest in the development of a new class of proteasome inhibitors. In this chapter, we discuss recent efforts towards the development of proteasome inhibitors. In addition, we discuss a novel class of compounds targeting an alternative proteasome, the immunoproteasome.
Original language | English |
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Title of host publication | Modulation of Protein Stability in Cancer Therapy |
Pages | 99-119 |
Number of pages | 21 |
DOIs | |
State | Published - 2009 |
Keywords
- Catalytic β-subunits
- Immunoproteasome-specific inhibitors, Activity-based probes
- N-terminal nucleophile protease
- Pharmacophores
- Proteasome inhibitors
- Subunit-specific inhibitors
- Ubiquitin-proteasome system
ASJC Scopus subject areas
- General Biochemistry, Genetics and Molecular Biology