Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate

Abstract ADAM10 and ADAM17 have been shown to contribute to the acquired drug resistance of HER2-positive breast cancer in response to trastuzumab. The majority of ADAM10 and ADAM17 inhibitor development has been focused on the discovery of compounds that bind the active site zinc, however, in recen...

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Bibliographic Details
Main Authors: Franck Madoux, Daniela Dreymuller, Jean-Phillipe Pettiloud, Radleigh Santos, Christoph Becker-Pauly, Andreas Ludwig, Gregg B. Fields, Thomas Bannister, Timothy P. Spicer, Mare Cudic, Louis D. Scampavia, Dmitriy Minond
Format: Article
Language:English
Published: Nature Publishing Group 2016-12-01
Series:Scientific Reports
Online Access:https://doi.org/10.1038/s41598-016-0013-4