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  • Function-oriented biosynthesis of beta-lactone proteasome inhibitors in Salinispora tropica.

Function-oriented biosynthesis of beta-lactone proteasome inhibitors in Salinispora tropica.

Journal of medicinal chemistry (2009-09-15)
Markus Nett, Tobias A M Gulder, Andrew J Kale, Chambers C Hughes, Bradley S Moore
ABSTRACT

The natural proteasome inhibitor salinosporamide A from the marine bacterium Salinispora tropica is a promising drug candidate for the treatment of multiple myeloma and mantle cell lymphoma. Using a comprehensive approach that combined chemical synthesis with metabolic engineering, we generated a series of salinosporamide analogues with altered proteasome binding affinity. One of the engineered compounds is equipotent to salinosporamide A in inhibition of the chymotrypsin-like activity of the proteasome yet exhibits superior activity in the cell-based HCT-116 assay.

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(Bromomethyl)cyclobutane, 97%