Xia, Liqun and Lin, Haili and Staniek, Agata and Panjikar, and Ruppert, Martin and Hilgers, Petra and Williardt, Joerg and Rajendran, Chitra and Wang, Meitian and Warzecha, Heribert and Jaeger, Volker and Stoeckigt, Joachim (2015) Ligand structures of synthetic deoxa-pyranosylamines with raucaffricine and strictosidine glucosidases provide structural insights into their binding and inhibitory behaviours. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 30 (3). pp. 472-478. ISSN 1475-6366, 1475-6374
Full text not available from this repository. (Request a copy)Abstract
Insight into the structure and inhibition mechanism of O-beta-D-glucosidases by deoxa-pyranosylamine type inhibitors is provided by X-ray analysis of complexes between raucaffricine and strictosidine glucosidases and N-(cyclohexylmethyl)-, N-(cyclohexyl)- and N-(bromobenzyl)-beta-D-gluco-1,5-deoxa-pyranosylamine. All inhibitors anchored exclusively in the catalytic active site by competition with appropriate enzyme substrates. Thus facilitated prospective elucidation of the binding networks with residues located at <3.9 angstrom distance will enable the development of potent inhibitors suitable for the production of valuable alkaloid glucosides, raucaffricine and strictosidine, by means of synthesis in Rauvolfia serpentina cell suspension cultures.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | POTENT GLYCOSIDASE INHIBITORS; BETA-GLUCOSIDASES; MANNOSTATIN-A; EMERGING CLASS; AMINO(HYDROXYMETHYL)CYCLOPEN-TANETRIOLS; BIOSYNTHESIS; MANNOSIDASE; EXPRESSION; HYDROLASES; ALKALOIDS; Crystallization; glucosidase inhibition; structure elucidation |
| Subjects: | 600 Technology > 610 Medical sciences Medicine |
| Divisions: | Chemistry and Pharmacy > Institut für Organische Chemie |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 11 Jul 2019 13:00 |
| Last Modified: | 11 Jul 2019 13:00 |
| URI: | https://pred.uni-regensburg.de/id/eprint/5374 |
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