Non-Covalent Inhibitors of the 20S Proteasome
DOI:
https://doi.org/10.2533/000942903777679415Keywords:
Antitumor agents, Drug design, Enzyme inhibitors, PeptidomimeticAbstract
Peptidomimetics have been commonly used as lead compounds to design inhibitors with high affinity and specificity for a particular enzyme. The discovery that a 2-aminobenzylstatine derivative originally designed to target an aspartyl protease was able to inhibit specifically and non-covalently the chymotrypsin-like activity of the 20S proteasome represented a unique starting point for our medicinal chemistry endeavor for this target. Utilizing a structure-based design approach, we have been able to improve the potency of this new class of proteasome inhibitors without affecting its in vitro selectivity profile.Downloads
Published
2003-04-01
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Scientific Articles
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Copyright (c) 2003 Swiss Chemical Society
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
How to Cite
[1]
Chimia 2003, 57, 179, DOI: 10.2533/000942903777679415.