Nicotinic Acetylcholine Receptor Agonists: A Milestone for Modern Crop Protection
Identifieur interne : 001142 ( Main/Exploration ); précédent : 001141; suivant : 001143Nicotinic Acetylcholine Receptor Agonists: A Milestone for Modern Crop Protection
Auteurs : Peter Jeschke [Allemagne] ; Ralf Nauen [Allemagne] ; Michael Edmund Beck [Allemagne]Source :
- Angewandte Chemie International Edition [ 1433-7851 ] ; 2013-09-02.
English descriptors
- Teeft :
- Abstr, Acetylcholine, Achbp, Achbps, Ache inhibitors, Active ingredients, Agonist, Agric, Analogue, Angew, Angewandte, Angewandte chemie nicotinic acetylcholine receptor agonists, Angewandte reviews, Aphid, Appl, Application methods, Bayer, Bayer cropscience, Beck, Beltwide cotton conf, Binding affinity, Binding mode, Binding modes, Binding site, Bioactive scaffold, Biochem, Biol, Biological profile, Butenolide, Casida, Chem, Chemie, Clothianidin, Commercial agonists, Common name, Crop protection, Cropscience, Crystal structures, Electron density, Extracellular, Extracellular domain, Foliar, Foliar application, Food chem, Fukui, Fukui function, Fukui functions, Functional architecture, Gmbh, Green peach aphid, Green rice, High target specificity, Homology, Homology models, Homopentameric achbps, Hydrogen bond, Imidacloprid, Insect nachrs, Insecticidal, Insecticidal activity, Insecticide, Jeschke, Kagabu, Kgaa, Ligand, Ligand binding, Mammalian nachrs, Modern crop protection, Modern crop protection compounds, Modern insecticides, Moiety, Mutation, Nachr, Nachr agonists, Nachr subunits, Nachrs, Nauen, Neonicotinoid, Neonicotinoid insecticides, Neonicotinoids, Nicotinic, Nicotinic acetylcholine receptor, Nicotinic acetylcholine receptors, Nihon tokushu noyaku seizo, Nippon soda, Nitrogen atom, Noncyclic, Noncyclic structures, Novel nachr agonists, Optimization procedure, Other hand, Persicae, Persicae sulzer, Pest, Pestic, Pharmacophore, Physicochemical, Physicochemical properties, Phytotonic effects, Proc, Pyridine ring, Rational design, Recent trends, Receptor, Receptor domain, Ring systems, Sattelle, Schirmer, Seed treatment, Selectivity, Shao, Springer, Stemofoline, Subunit, Sulfoximine, Sulfoximine core, Sulzer, Tomizawa, Toxicity, Utmost importance, Verlag, Verlag gmbh, Virtual screening, Virus diseases, Weinheim, Weinheim angew, Whitefly, Witschel.
Abstract
The destruction of crops by invertebrate pests is a major threat against a background of a continuously rising demand in food supply for a growing world population. Therefore, efficient crop protection measures in a vast range of agricultural settings are of utmost importance to guarantee sustainable yields. The discovery of synthetic agonists selectively addressing the nicotinic acetylcholine receptors (nAChRs), located in the central nervous system of insects, for use as insecticides was a major milestone in applied crop protection research. These compounds, as a result of their high target specificity and versatility in application methods, opened a new innovative era in the control of some of the world′s most devastating insect pests. These insecticides also contributed massively to extending our knowledge of the biochemistry of insect nicotinic acetylcholine receptors. The global economic success of synthetic nAChR agonists as insecticides renders the nicotinic acetylcholine receptor still one of the most attractive target sites for exploration in insecticide discovery.
Sustainable agriculture: The discovery of neonicotinoid insecticides can be considered a milestone in crop protection research. As potent agonists selectively acting on insect nicotinic acetylcholine receptors, they also contributed to the understanding of nicotinic receptors of insects (see picture; left: superposition of various neonicotinoids; right: binding of a neonicotinoid to a receptor with an R81T mutation).
Url:
DOI: 10.1002/anie.201302550
Affiliations:
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<term>Agonist</term>
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<term>Bayer cropscience</term>
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<term>Binding mode</term>
<term>Binding modes</term>
<term>Binding site</term>
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<term>Biol</term>
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<term>Casida</term>
<term>Chem</term>
<term>Chemie</term>
<term>Clothianidin</term>
<term>Commercial agonists</term>
<term>Common name</term>
<term>Crop protection</term>
<term>Cropscience</term>
<term>Crystal structures</term>
<term>Electron density</term>
<term>Extracellular</term>
<term>Extracellular domain</term>
<term>Foliar</term>
<term>Foliar application</term>
<term>Food chem</term>
<term>Fukui</term>
<term>Fukui function</term>
<term>Fukui functions</term>
<term>Functional architecture</term>
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<term>Green peach aphid</term>
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<front><div type="abstract" xml:lang="en">The destruction of crops by invertebrate pests is a major threat against a background of a continuously rising demand in food supply for a growing world population. Therefore, efficient crop protection measures in a vast range of agricultural settings are of utmost importance to guarantee sustainable yields. The discovery of synthetic agonists selectively addressing the nicotinic acetylcholine receptors (nAChRs), located in the central nervous system of insects, for use as insecticides was a major milestone in applied crop protection research. These compounds, as a result of their high target specificity and versatility in application methods, opened a new innovative era in the control of some of the world′s most devastating insect pests. These insecticides also contributed massively to extending our knowledge of the biochemistry of insect nicotinic acetylcholine receptors. The global economic success of synthetic nAChR agonists as insecticides renders the nicotinic acetylcholine receptor still one of the most attractive target sites for exploration in insecticide discovery.</div>
<div type="abstract" xml:lang="en">Sustainable agriculture: The discovery of neonicotinoid insecticides can be considered a milestone in crop protection research. As potent agonists selectively acting on insect nicotinic acetylcholine receptors, they also contributed to the understanding of nicotinic receptors of insects (see picture; left: superposition of various neonicotinoids; right: binding of a neonicotinoid to a receptor with an R81T mutation).</div>
</front>
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