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Order and disorder: differential structural impacts of myricetin and ethyl caffeate on human amylase, an antidiabetic target.

Abstract：

:The increasing prevalence of diabetes has accelerated the search for new drugs derived from natural sources. To define the functional features of two such families of compounds, the flavonols and the ethyl caffeates, we have determined the high-resolution structures of representative inhibitors in complex with human pancreatic α-amylase. Myricetin binds at the active site and interacts directly with the catalytic residues despite its bulky planar nature. Notably, it reduces the normal conformational flexibility of the adjacent substrate binding cleft. In contrast, bound ethyl caffeate acts by disordering precisely those polypeptide chain segments that make up the active site binding cleft. It also operates from binding sites far removed from the active site, a property not observed in any other class of human α-amylase inhibitor studied to date. Given the current inadequacy of drugs directed at diabetes, the use of optimized flavonols and ethyl caffeates may present an alternative therapeutic route.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Williams LK,Li C,Withers SG,Brayer GD

doi

10.1021/jm301273u

subject

Has Abstract

pub_date

2012-11-26 00:00:00

pages

10177-86

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

55

pub_type

杂志文章

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