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Open Access Protoporphyrinogen Oxidase Inhibitor: An Ideal Target for Herbicide Discovery

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As the last common enzyme in the biosynthetic pathway leading to heme and chlorophyll, protoporphyrinogen oxidase (PPO; EC 1.3.3.4) is an ideal target for herbicide development. Currently, about 30 PPO inhibitors have been developed as agricultural herbicides. PPO inhibitors have displayed environmentally benign, but advantageous characteristics, including low toxicity, low effective concentration, broad herbicidal spectrum (active against both monocotyledon and dicotyledon weeds), quick onset of action, and long lasting effect. Over the last several years, great achievements have been made in revealing the structural biology of PPO. Five PPO crystal structures, four isolated in enzyme-inhibitor complexes and one in the native form, have been determined, including those from Nicotiana tabacum, Myxococcus Xanthus, Bacillus subtilis, and human. Although PPO inhibitors have been developed for over forty years, we continue to uncover exciting future prospects for novel PPO-inhibiting herbicides. In this review, we have summarized the structures of PPOs from plants, human, and bacteria; the interactions between PPOs and inhibitors; the quantitative structure–activity relationships of PPO inhibitors; and the molecular design of new PPO inhibitors.

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Keywords: HERBICIDE; INHIBITOR; MOLECULAR DESIGN; PROTOPORPHYRINOGEN OXIDASE; QSAR

Document Type: Research Article

Affiliations: 1: College of Chemistry, Central China Normal University Key Laboratory of Pesticide & Chemical Biology of Ministry of Education Wuhan 430079, P. R. China 2: College of Chemistry, Central China Normal University Key Laboratory of Pesticide & Chemical Biology of Ministry of Education Wuhan 430079, P. R. China. [email protected]

Publication date: December 1, 2011

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  • International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions

    CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.

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