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Article

Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice

23 Sept 2015

Abstract excerpt

Insulin-degrading enzyme (IDE) is a protease that cleaves insulin and other bioactive peptides such as amyloid-β. Knockout and genetic studies have linked IDE to Alzheimer's disease and type-2 diabetes. As the major insulin-degrading protease, IDE is a candidate drug target in diabetes. Here we have used kinetic target-guided synthesis to design the first catalytic site inhibitor of IDE suitable for in vivo...

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PMID: 26394692
DOI: 10.1038/ncomms9250

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