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(−)-Homosalinosporamide A and Its Mode of Proteasome Inhibition: An X-ray Crystallographic Study

Upon acylation of the proteasome by the β-lactone inhibitor salinosporamide A (SalA), tetrahydrofuran formation occurs by intramolecular alkylation of the incipient alkoxide onto the choroethyl sidechain and irreversibly blocks the active site. Our previously described synthetic approach to SalA, ut...

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Detalhes bibliográficos
Publicado no:Mar Drugs
Main Authors: Groll, Michael, Nguyen, Henry, Vellalath, Sreekumar, Romo, Daniel
Formato: Artigo
Idioma:Inglês
Publicado em: MDPI 2018
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6071143/
https://ncbi.nlm.nih.gov/pubmed/30029468
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.3390/md16070240
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