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

Travis Coyle; Aleksandra W. Debowski; Annabelle Varrot; Keith A. Stubbs

doi:10.1002/cbic.201700073

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

Travis Coyle
, Aleksandra W. Debowski
, Annabelle Varrot
, Keith A. Stubbs

Research output: Contribution to journal › Article › peer-review

1 Citation (Web of Science)

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.

Original language	English
Pages (from-to)	974-978
Number of pages	5
Journal	ChemBioChem
Volume	18
Issue number	11
DOIs	https://doi.org/10.1002/cbic.201700073
Publication status	Published - 1 Jun 2017

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10.1002/cbic.201700073

https://rss.onlinelibrary.wiley.com/doi/am-pdf/10.1002/cbic.201700073

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

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",

author = "Travis Coyle and Debowski, \{Aleksandra W.\} and Annabelle Varrot and Stubbs, \{Keith A.\}",

year = "2017",

month = jun,

day = "1",

doi = "10.1002/cbic.201700073",

language = "English",

volume = "18",

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AU - Coyle, Travis

AU - Debowski, Aleksandra W.

AU - Varrot, Annabelle

AU - Stubbs, Keith A.

PY - 2017/6/1

Y1 - 2017/6/1

N2 - 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.

AB - 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.

KW - arabinanases

KW - carbamate

KW - chromogenic substrate

KW - enzyme inhibitors

KW - hydroximolactone

UR - https://www.scopus.com/pages/publications/85018549752

U2 - 10.1002/cbic.201700073

DO - 10.1002/cbic.201700073

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EP - 978

JO - ChemBioChem

JF - ChemBioChem

IS - 11

ER -

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

Abstract

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Using Genetic Tools to Study Helicobacter Pylori & Persistence

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

Abstract

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Using Genetic Tools to Study Helicobacter Pylori & Persistence

The Development of Tools to Study Carbohydrate-Processing Enzymes Implicated in Human Disease

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