Research output: Contribution to journal › Article › peer-review
Journal | Angewandte Chemie International Edition |
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Date | E-pub ahead of print - 6 Dec 2015 |
Date | Published (current) - 14 Dec 2015 |
Number of pages | 6 |
Early online date | 6/12/15 |
Original language | English |
Pyrrolidine-based iminocyclitols are a promising class of glycosidase inhibitors. Reported herein is a convenient epimerization strategy that provides direct access to a range of stereoisomeric iminocyclitol inhibitors of O-GlcNAcase (OGA), the enzyme responsible for catalyzing removal of O-GlcNAc from nucleocytoplasmic proteins. Structural details regarding the binding of these inhibitors to a bacterial homologue of OGA reveal the basis for potency. These compounds are orally available and permeate into rodent brain to increase O-GlcNAc, and should prove useful tools for studying the role of OGA in health and disease.
© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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