Development of smart drugs for the sensing and inhibition of target biomolecules

2022 Fiscal Year Final Research Report

• Project/Area Number: 21K19317
• Research Category: Grant-in-Aid for Challenging Research (Exploratory)
• Allocation Type: Multi-year Fund
• Review Section: Medium-sized Section 47:Pharmaceutical sciences and related fields
• Research Institution: Kyoto Institute of Technology
• Principal Investigator: Matsuo Kazuya 京都工芸繊維大学, 分子化学系, 助教 (90764952)
• Project Period (FY): 2021-07-09 – 2023-03-31
• Keywords: 分子内転位反応 / スマートドラッグ

Outline of Final Research Achievements

The half of the drugs we clinically use nowadays are enzyme inhibitors which can exhibit their effects through the specific binding to the target enzymes. Since the target enzymes are considerably expressed even in normal cells and tissues, severe side effects can be induced due to inhibiting the enzymes. To solve this significant drawback, we have developed a molecular system to release the inhibitors depending on the activities of target enzymes based on the intramolecular reaction. Also, we have developed the photoswitchable drugs that can be controlled by light with high spatiotemporal resolution.

Free Research Field

ケミカルバイオロジー

Academic Significance and Societal Importance of the Research Achievements

本研究によって得られた分子内転位反応を利用した阻害剤構築法によって、副作用を減弱できうる機能性薬剤「スマートドラッグ」の新規デザイン法が確立され、創薬技術ならびに創薬戦略の向上・発展に貢献できる。また、光制御型ROCK阻害剤の開発およびその成果を通じて、全身毒性を大きく抑えた状態で、疾患部位特異的に光で作用させる次世代の光薬剤治療法（光薬理学）の発展にも大きく貢献できる。