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Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic α-amylase

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Abstract

Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, KI = 60 and 70 nM, with improved specificity over medically relevant glycosidases, making them promising candidates for controlling blood glucose. Crystallographic analysis confirmed similar binding modes and identified new active site interactions.

Graphical abstract: Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic α-amylase

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Publication details

The article was received on 29 May 2019, accepted on 16 Oct 2019 and first published on 18 Oct 2019


Article type: Edge Article
DOI: 10.1039/C9SC02610J
Chem. Sci., 2019, Advance Article
  • Open access: Creative Commons BY-NC license
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    Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic α-amylase

    C. R. Tysoe, S. Caner, M. B. Calvert, A. Win-Mason, G. D. Brayer and S. G. Withers, Chem. Sci., 2019, Advance Article , DOI: 10.1039/C9SC02610J

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