Incorporation of Non-natural Amino Acids Improves Cell Permeability and Potency of Specific Inhibitors of Proteasome Trypsin-like Sites

Proteasomes degrade the majority of proteins in mammalian cells by a concerted action of three distinct pairs of active sites. The chymotrypsin-like sites are targets of antimyeloma agents bortezomib and carfilzomib. Inhibitors of the trypsin-like site sensitize multiple myeloma cells to these agent...

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Main Authors: Geurink, Paul P., van der Linden, Wouter A., Mirabella, Anne C., Gallastegui, Nerea, de Bruin, Gerjan, Blom, Annet E. M., Voges, Mathias J., Mock, Elliot D., Florea, Bogdan I., van der Marel, Gijs A., Driessen, Christoph, van der Stelt, Mario, Groll, Michael, Overkleeft, Herman S., Kisselev, Alexei F.
Formato: Artigo
Idioma:Inglês
Publicado em: 2013
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3782865/
https://ncbi.nlm.nih.gov/pubmed/23320547
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm3016987
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