Dry and wet approach for the disclosure of the interaction between ecdysone receptor and ligand molecule

2015 Fiscal Year Final Research Report

• Project/Area Number: 25450070
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Plant protection science
• Research Institution: Kyoto University
• Principal Investigator: NAKAGAWA Yoshiaki 京都大学, (連合)農学研究科(研究院), 准教授 (80155689)
• Co-Investigator(Renkei-kenkyūsha): MINAKUCHI Chieka 名古屋大学, 大学院生命農学研究科, 助教 (90509134)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: ecdysoone / ponasterone A / ecdysone receptor / diacylhydrazine / 20-hydroxyecdysone / imidazole / tetrahydroquinoline / Bemisia tabaci

Outline of Final Research Achievements

Molting hormone agonists with varied basic structures, such as diacylhydrazine, imidazole, imidazothiadiazole, tetrahydroquinoline, were chemically synthesized and their binding affinity to varied ecdysone receptors (EcRs) was quantitatively measured. Effect of the alkyl substituents of the imidazole ring on the binding affinity against Spodoptera furugiperda EcR was studied. With respect to imidazothiadiazole analogs, the substituent effects were quantitatively analyzed using QSAR. Racemic cis-form of a tetrahydroquinoline analog was separated into two enantiomers and their absolute configurations were determined. The binding affinity of these two enantiomers was evaluated against Aedes albopictus. Amino acid sequences of EcRs of two ladybug species and a sweet potato whitefly were deduced using cDNA cloning. Ligand-receptor binding assay was performed using these in vitro translated EcR and USP.

Free Research Field

生物調節化学，農薬化学