Peptido sulfonyl fluorides as new powerful proteasome inhibitors

Brouwer, A.J. et al. (2012) Peptido sulfonyl fluorides as new powerful proteasome inhibitors. Journal of Medicinal Chemistry, 55(24), pp. 10995-11003. (doi: 10.1021/jm301443r)

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A new class of potent proteasome inhibitors is described, of which the members contain an amino acid inspired sulfonyl fluoride as the electrophilic trap. In total, 24 peptido sulfonyl fluoride inhibitors have been designed and synthesized, which were inspired by the backbone sequences of the proteasome inhibitors bortezomib, epoxomicin, and Cbz-Leu3-aldehyde. Nine of them were very potent proteasome inhibitors, the best of which had an IC50 of 7 nM. A number of the peptido sulfonyl fluoride inhibitors were found to be highly selective for the β5 proteasome subunit.

Item Type:Articles
Glasgow Author(s) Enlighten ID:Liskamp, Professor Robert
Authors: Brouwer, A.J., Jonker, A., Werkhoven, P., Kuo, E., Li, N., Gallastegui, N., Kemmink, J., Florea, B.I., Groll, M., Overkleeft, H.S., and Liskamp, R.M.J.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Journal of Medicinal Chemistry
Publisher:American Chemical Society

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