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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Auteurs principaux: 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
Langue:Inglês
Publié: American Society for Biochemistry and Molecular Biology 2010
Sujets:
Protein Synthesis and Degradation
Accès en ligne: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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