Novel N-substituted 5-phosphate-d-arabinonamide derivatives as strong inhibitors of phosphoglucose isomerases: Synthesis, structure-activity relationship and crystallographic studies.

Bioorganic Chemistry(2020)

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摘要
•New inhibitors of the cancer biomarker AMF-hPGI obtained from a common precursor.•Although not HEI analogues, some ligands display strong inhibition properties.•Crystal structure of human PGI in complex with an inhibitor resolved at 2.38 Å.•The active site of AMF-hPGI is tolerant towards the “C-1” part of the inhibitor.
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关键词
Enzyme inhibitor,Phosphate,Monosaccharide,Phosphoglucose isomerase,Autocrine motility factor
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