Nature of Pharmacophore Influences Active Site Specificity of Proteasome Inhibitors

Proteasomes degrade most proteins in mammalian cells and are established targets of anti-cancer drugs. The majority of proteasome inhibitors are composed of short peptides with an electrophilic functionality (pharmacophore) at the C terminus. All eukaryotic proteasomes have three types of active sit...

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Main Authors: Screen, Michael, Britton, Matthew, Downey, Sondra L., Verdoes, Martijn, Voges, Mathias J., Blom, Annet E. M., Geurink, Paul P., Risseeuw, Martijn D. P., Florea, Bogdan I., van der Linden, Wouter A., Pletnev, Alexandre A., Overkleeft, Herman S., Kisselev, Alexei F.
Format: Artigo
Jezik:Inglês
Izdano: American Society for Biochemistry and Molecular Biology 2010
Teme:
Protein Synthesis and Degradation
Online dostop:https://ncbi.nlm.nih.gov/pmc/articles/PMC3000995/
https://ncbi.nlm.nih.gov/pubmed/20937826
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.M110.160606
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