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The structure-activity relationship of the salicylimide derived inhibitors of UDP-sugar producing pyrophosphorylases
Umeå University, Faculty of Science and Technology, Department of Plant Physiology. Umeå University, Faculty of Science and Technology, Umeå Plant Science Centre (UPSC).
Umeå University, Faculty of Science and Technology, Department of Chemistry.ORCID iD: 0000-0002-8804-829X
Umeå University, Faculty of Science and Technology, Department of Plant Physiology. Umeå University, Faculty of Science and Technology, Umeå Plant Science Centre (UPSC).ORCID iD: 0000-0001-8685-9665
2018 (English)In: Plant Signalling & Behavior, ISSN 1559-2316, E-ISSN 1559-2324, Vol. 13, no 8, article id e1507406Article in journal (Refereed) Published
Abstract [en]

UDP-sugars are key precursors for biomass production in nature (synthesis of cellulose, hemicellulose, etc.). They are produced de novo by distinct UDP-sugar producing pyrophosphorylases. Studies on the roles of these enzymes using genetic knockouts were hampered by sterility of the mutants and by functional-complementation from related enzyme(s), hindering clear interpretation of the results. In an attempt to override these difficulties, we turned to the reverse chemical genetics approaches to identify compounds which interfere with the activity of those enzymes in vivo. Hit expansion on one of such compounds, a salicylimide derivative, allowed us to identify several inhibitors with a range of activities. The present study provides a structure-activity relationship for these compounds.

Place, publisher, year, edition, pages
Taylor & Francis, 2018. Vol. 13, no 8, article id e1507406
Keywords [en]
Enzyme inhibition, reverse chemical genetics, UDP-N-acetyl glucosamine pyrophosphorylase, UDP- ucose pyrophosphorylase, UDP-sugar pyrophosphorylase
National Category
Biochemistry and Molecular Biology Botany
Identifiers
URN: urn:nbn:se:umu:diva-152288DOI: 10.1080/15592324.2018.1507406ISI: 000444498100025PubMedID: 30125142OAI: oai:DiVA.org:umu-152288DiVA, id: diva2:1252305
Available from: 2018-10-01 Created: 2018-10-01 Last updated: 2018-10-01Bibliographically approved

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Decker, DanielÖberg, ChristopherKleczkowski, Leszek A.

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Decker, DanielÖberg, ChristopherKleczkowski, Leszek A.
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Department of Plant PhysiologyUmeå Plant Science Centre (UPSC)Department of Chemistry
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