Open AccessHarnessing Proteasome Dynamics and Allostery in Drug Design
Author(s) -
Maria Gaczyńska,
Paweł A. Osmulski
Publication year - 2014
Publication title -
antioxidants and redox signaling
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.277
H-Index - 190
eISSN - 1557-7716
pISSN - 1523-0864
DOI - 10.1089/ars.2013.5816
Subject(s) - allosteric regulation , proteasome , biology , protease , small molecule , drug discovery , ubiquitin , microbiology and biotechnology , computational biology , biophysics , biochemistry , enzyme , gene
The proteasome is the essential protease that is responsible for regulated cleavage of the bulk of intracellular proteins. Its central role in cellular physiology has been exploited in therapies against aggressive cancers where proteasome-specific competitive inhibitors that block proteasome active centers are very effectively used. However, drugs regulating this essential protease are likely to have broader clinical usefulness. The non-catalytic sites of the proteasome emerge as an attractive alternative target in search of highly specific and diverse proteasome regulators.