Inhibition of plant glutamine synthetases by substituted phosphinothricins.

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 Physiol

journal_title

Plant physiology

authors

Logusch EW,Walker DM,McDonald JF,Franz JE

doi

10.1104/pp.95.4.1057

subject

Has Abstract

pub_date

1991-04-01 00:00:00

pages

1057-62

issue

4

eissn

0032-0889

issn

1532-2548

journal_volume

95

pub_type

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