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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Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: American Society for Biochemistry and Molecular Biology 2010
Témata:
Protein Synthesis and Degradation
On-line přístup: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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