An Enzyme-Targeted Herbicide Design Program Based on EPSP Synthase: Chemical Mechanism and Glyphosate Inhibition Studies

  • James A. Sikorski
  • Karen S. Anderson
  • Darryl G. Cleary
  • Michael J. Miller
  • Paul D. Pansegrau
  • Joel E. Ream
  • R. Douglas Sammons
  • Kenneth A. Johnson
Part of the Industry-University Cooperative Chemistry Program Symposia book series (IUCC)


The herbicide markets of the late 1990’s and beyond will demand high performance products with stringent environmental acceptability requirements. We have initiated a multi-disciplinary herbicide discovery program directed toward the inhibition of key plant enzymes as one approach to meet these challenges. Plants contain a variety of biosynthetic pathways which are essential for their growth. Effective, plant-specific enzyme inhibitors offer the opportunity to satisfy the herbicide performance needs of the marketplace while exhibiting favorably low mammalian toxicity properties.1 Our enzyme-targeted research effort systematically integrates mechanistic biochemistry, molecular biology, modeling, inhibitor recognition, and structural biology information with organic synthesis through a series of collaborations within and outside Monsanto. A thorough understanding of the chemical mechanism for a particular enzyme target is an essential first step for the design of potent inhibitors.


Ternary Complex Vinyl Ether Internal Equilibrium Tetrahedral Intermediate Minor Structural Change 


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Copyright information

© Springer Science+Business Media New York 1990

Authors and Affiliations

  • James A. Sikorski
    • 1
  • Karen S. Anderson
    • 2
  • Darryl G. Cleary
    • 1
  • Michael J. Miller
    • 1
  • Paul D. Pansegrau
    • 1
  • Joel E. Ream
    • 1
  • R. Douglas Sammons
    • 1
  • Kenneth A. Johnson
    • 2
  1. 1.Technology DivisionMonsanto Agricultural Company, A Unit of Monsanto CompanySt. LouisUSA
  2. 2.Departments of Molecular & Cell Biology and ChemistryThe Pennsylvania State Univ.University ParkUSA

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