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Unique neonicotinoid binding conformations conferring selective receptor interactions.

Motohiro Tomizawa1, John E Casida

  • 1Faculty of Education, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan. mtomizaw@gifu-u.ac.jp

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Neonicotinoids target insect nicotinic acetylcholine receptors (nAChRs) selectively. Differences in how neonicotinoids bind to acetylcholine binding proteins (AChBPs) explain this specificity, revealing unique receptor interactions.

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Area of Science:

  • Neuroscience
  • Molecular Biology
  • Pharmacology

Background:

  • Neonicotinoids are insecticides that target insect nicotinic acetylcholine receptors (nAChRs).
  • Acetylcholine binding proteins (AChBPs) are structural homologues of nAChRs, useful for studying ligand-receptor interactions.
  • Distinct pharmacological profiles of Aplysia AChBP (high neonicotinoid sensitivity) and Lymnaea AChBP (low sensitivity) mimic insect and vertebrate nAChR subtypes.

Purpose of the Study:

  • To elucidate the molecular basis for neonicotinoid selectivity at the nicotinic acetylcholine receptor.
  • To compare ligand-receptor interactions of neonicotinoids and nicotinoids with Aplysia and Lymnaea AChBPs.

Main Methods:

  • Utilized chemical and structural neurobiology approaches.
  • Compared binding conformations of neonicotinoids and nicotinoids with Aplysia AChBP and Lymnaea AChBP.

Main Results:

  • Neonicotinoids and nicotinoids bind in a single conformation with Aplysia AChBP.
  • Neonicotinoids exhibit two inverted binding conformations with Lymnaea AChBP, while nicotinoids bind in one.
  • The orientation of the pharmacophore (nitro/cyano group) differs between neonicotinoids and nicotinoids in Aplysia AChBP.

Conclusions:

  • Unique binding conformations of nicotinic agonists are critical for selective receptor interactions.
  • Understanding these interactions can inform the design of more selective insecticides.
  • Structural differences in AChBPs explain differential neonicotinoid sensitivity, mirroring nAChR subtypes.