Screen of insect growth regulators that inhibit the novel ecdysteroidogenic enzyme

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K14719
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Bioorganic chemistry
• Research Institution: University of Tsukuba
• Principal Investigator: NIWA Ryusuke 筑波大学, 生命環境系, 准教授 (60507945)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: 農薬 / 昆虫 / 酵素 / エクジステロイド / グルタチオンS-転移酵素

Outline of Final Research Achievements

This study aims to identify novel insect growth regulators that inhibit the enzymatic activity of Noppera-bo, a glutathione S-transferase essential for ecdysteroid biosynthesis. We utilized our own high-throughput chemical screen system and identified several candidate compounds, including β-estradiol. X-ray crystallographic and biochemical analyses revealed that the inhibitory effect of β-estradiol requires a specific hydrogen bond interaction between β-estradiol and Noppera-bo. Our results provide a novel insight into a design principle for developing practical insect growth regulators impairing ecdysteroid biosynthesis in the future.

Free Research Field

昆虫生理学