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

ABSTRACT: Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, K I = 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.

SUBMITTER: Tysoe CR

PROVIDER: S-EPMC7069248 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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

Tysoe Christina R CR Caner Sami S Calvert Matthew B MB Win-Mason Anna A Brayer Gary D GD Withers Stephen G SG

Chemical science 20191018 48

Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, K I = 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. ...[more]

PMID: 32206255

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