@techreport{oai:kindai.repo.nii.ac.jp:00019715, author = {伊原, 誠 and 疋田, 麻衣 and 福田, 芳恵}, month = {}, note = {研究成果の概要(和文):ネオニコチノイド系殺虫剤は,世界中で広く使用されている農業・園芸用殺虫剤であり,近年その毒性に注目が集まっている.本研究では,ネオニコチノイドの毒性発現を制御するニコチン性アセチルコリン受容体(nAChR)の構造因子を探索するために,nAChRのモデルタンパク質,アセチルコリン結合タンパク質を用いたX線結晶構造解析およびホモロジーモデリング法を用いて,ネオニコチノイドとnAChRの相互作用に重要な構造因子を探索した.その結果,昆虫のnAChRαサブユニット上に存在する,Loop領域のうちD,G,E領域のアミノ酸残基がネオニコチノイドとの相互作用に有利な構造を形成することを明らかにした. 研究成果の概要(英文):Neonicotinoids are widely used for crop protection and veterinary use worldwilde. Recently the adverse effects of neonicotinoids have been focused, and some of them were banned from EU. In order to elucidate the molecular mechanism of such adverse effects of neonicotinoids, X-ray crystallography of acetylcholine binding protein, a surrogate protein of ligand binding domain of nicotinic acetylcholine receptors, has been employed and the X-ray crystal structures of AChBP-neonicotinoids complexes were solved. Using those structures, homology models were built and evaluated their interactions. These results suggested that LOOPs D, E and G cooperatively form neonicotinoid-fovored environment in insect nAChRs. Physiological evaluation confirmed that even single mutation at the Loop D, E and G strikingly weakened the neonicotinoid actions on insect nAChRs. These results suggest the adverse effects of neonicotinoids might be controlled through structure guided approaches., 研究種目:若手研究(B); 研究期間:2016~2017; 課題番号:16K21507; 研究分野:農薬科学; 科研費の分科・細目:, application/pdf}, title = {ネオニコチノイドの毒性発現を制御するニコチン性アセチルコリン受容体の構造因子探索}, year = {2018}, yomi = {イハラ, マコト and ヒキダ, マイ and ユクタ, ヨシエ} }