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Probing the aglycon binding site of a beta-glucosidase: a collection of C-1-modified 2,5-dideoxy-2,5-imino-D-mannitol derivatives and their structure-activity relationships as competitive inhibitors

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  • Tanja M Wrodnigg
  • Diness, Frederik
  • Christoph Gruber
  • Herwig Häusler
  • Inge Lundt
  • Karen Rupitz
  • Andreas J Steiner
  • Arnold E Stütz
  • Chris A Tarling
  • Stephen G Withers
  • Heidrun Wölfler

A range of new C-1 modified derivatives of the powerful glucosidase inhibitor 2,5-dideoxy-2,5-imino-D-mannitol has been synthesised and their biological activities probed with the beta-glucosidase from Agrobacterium sp. Ki values are compared with those of previously prepared close relatives. Findings suggest dramatic effects exerted by the aglycon binding site on substrate/inhibitor binding.

OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry
Vol/bind12
Udgave nummer13
Sider (fra-til)3485-95
Antal sider11
ISSN0968-0896
DOI
StatusUdgivet - 1 jul. 2004

ID: 158554721