Glyphosate is a very commonly-used, broad-spectrum herbicide. It is classifiied as a phosphonate, and it is systemic in activity. It is a non-selective herbicide used in agricultural research and plant biotechnology and forestry research applications. Its effectiveness as a herbicide was discovered by John Franz at Monsanto in 1970 and it was registered in the US in 1974 under the trade name Roundup.®
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|Mechanism of Action||
Glyphosate is an effective inhibitor of enolpyruvylshikinate-3-phosphate synthase (ESPS synthase), which is essential for the biosynthesis of select amino acids in plants, specifically three aromatic amino acids: tyrosine, tryptophan, and phenylalanine. The shikimate pathway that makes these is found in plants and microorganisms, but not animals or humans. Glyphosate is absorbed through foliage and minimally through roots, meaning that it is only effective on actively growing plants and does not prevent seed germination.
Glyphosate is a relatively simple molecule—an N-methyl phosphonate derivative of glycine with a chemical structure. Despite this simple structure, glyphosate retains specificity for EPSPS and is not known to inhibit any other enzyme.
Compound discovery studies with structure-based inhibitor design revealed that the binding of ligands to EPSPS causes a macroconformational change from an open form to a closed form of the enzyme. This could provide new templates for future efforts that target the design of novel antimicrobial and herbicidal agents that block enzyme closure and subsequent formation of the catalytic sites.
Broadleaf and woody weeds and grasses.
United States Environmental Protection Agency. "Glyphosate Fact Sheet"
Alibhai MF and Stallings WC (2001) Closing down on glyphosate inhibition--with a new structure for drug discovery. Proc Natl Acad Sci U S A. 98(6):2944-2946 PMID 11248008