The structure-activity relationship of the salicylimide derived inhibitors of UDP-sugar producing pyrophosphorylases. (3rd August 2018)

• Record Type: Journal Article
• Authors: Decker, Daniel; Öberg, Christopher; Kleczkowski, Leszek A.
• Is Part Of: Plant signaling & behavior. Volume 13:Number 8(2018)
• Publication Date: 2018-08-03
• Subjects: Enzyme inhibition -- reverse chemical genetics -- UDP-N-acetyl glucosamine pyrophosphorylase -- UDP-glucose pyrophosphorylase -- UDP-sugar pyrophosphorylase; Plant ecophysiology -- Periodicals; Plant cellular signal transduction -- Periodicals; Plant cellular signal transduction; Plant ecophysiology; Periodicals; Electronic journals; 581
• DOI: 10.1080/15592324.2018.1507406
• Languages: English
• ISSNs: 1559-2316

Abstract

ABSTRACT: 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.