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Chembiochem. 2017 Jun 1;18(11):974-978. doi: 10.1002/cbic.201700073. Epub 2017 Apr 20.

Exploiting sp2 -Hybridisation in the Development of Potent 1,5-α-l-Arabinanase Inhibitors.

Author information

1
School of Molecular Sciences, University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.
2
Present address: School of Chemistry, University College Dublin, Stillorgan Road, Belfield, Dublin, 4, Ireland.
3
School of Biomedical Sciences, University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.
4
CERMAV, Université Grenoble Alpes, CNRS, 38000, Grenoble, France.

Abstract

The synthesis of potent inhibitors of GH93 arabinanases as well as a synthesis of a chromogenic substrate to measure GH93 arabinanase activity are described. An insight into the reasons behind the potency of the inhibitors was gained through X-ray crystallographic analysis of the arabinanase Arb93A from Fusarium graminearum. These compounds lay a foundation for future inhibitor development as well as for the use of the chromogenic substrate in biochemical studies of GH93 arabinanases.

KEYWORDS:

arabinanases; carbamate; chromogenic substrate; enzyme inhibitors; hydroximolactone

PMID:
28266777
DOI:
10.1002/cbic.201700073
[Indexed for MEDLINE]

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