Abstract:
:Glutamine synthetase (GS) utilizes various substituted glutamic acids as substrates. We have used this information to design herbicidal alpha- and gamma-substituted analogs of phosphinothricin (l-2-amino-4-(hydroxymethylphosphinyl)butanoic acid, PPT), a naturally occurring GS inhibitor and a potent herbicide. The substituted phosphinothricins inhibit cytosolic sorghum GS(1) and chloroplastic GS(2) competitively versusl-glutamate, with K(i) values in the low micromolar range. At higher concentrations, these inhibitors inactivate glutamine synthetase, while dilution restores activity through enzyme-inhibitor dissociation. Herbicidal phosphinothricins exhibit low K(i) values and slow enzyme turnover, as described by reactivation characteristics. Both the GS(1) and GS(2) isoforms of plant glutamine synthetase are similarly inhibited by the phosphinothricins, consistent with the broad-spectrum herbicidal activity observed for PPT itself as well as other active compounds in this series.
journal_name
Plant Physioljournal_title
Plant physiologyauthors
Logusch EW,Walker DM,McDonald JF,Franz JEdoi
10.1104/pp.95.4.1057subject
Has Abstractpub_date
1991-04-01 00:00:00pages
1057-62issue
4eissn
0032-0889issn
1532-2548journal_volume
95pub_type
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