Screening for carbapenemase inhibitors among approved drug compounds

2016 Fiscal Year Final Research Report

• Project/Area Number: 16K15516
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Infectious disease medicine
• Research Institution: Nagoya University
• Principal Investigator: Arakawa Yoshichika 名古屋大学, 医学系研究科, 教授 (10212622)
• Co-Investigator(Renkei-kenkyūsha): KIMURA Kouji 名古屋大学, 大学院医学系研究科, 准教授 (50425675) ; WACHINO Jun-ichi 名古屋大学, 大学院医学系研究科, 講師 (00535651)
• Research Collaborator: JIN Wanchun 名古屋大学, 大学院医学系研究科, 特任助教 ; Kumar Anupuriya 名古屋大学, 大学院医学系研究科, 特任助教 ; YOKOYAMA Satoru 名古屋大学, 大学院医学系研究科 ; KANECHI Leo 名古屋大学, 大学院医学系研究科 ; KANAYAMA Takato 名古屋大学, 大学院医学系研究科
• Project Period (FY): 2016-04-01 – 2017-03-31
• Keywords: カルバペネマーゼ / 既承認薬 / ハイスループット / ニトロセフィン / 阻害剤

Outline of Final Research Achievements

Our object is to develop effective inhibitors of carbapenemases, β-lactamases with carbapenem hydrolyzing activity. In this study, we screened for carbapenemase inhibitors among 1018 approved drug compounds. To access this, high-throughput screening technique using purified carbapenemase, nitrocefin, and inhibitor candidate compounds, were developed. This HTS technique made us to evaluate the large number of compounds with ease and reliability in a short time. As a result, we could find 13 weak inhibitors, 11 intermediate inhibitors, and 9 strong inhibitors of one carbapenemase.

Free Research Field

細菌学