Drug discovery for targeting an mTORC component

2020 Fiscal Year Final Research Report

• Project/Area Number: 18K07329
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 50020:Tumor diagnostics and therapeutics-related
• Research Institution: Iwate Medical University
• Principal Investigator: Nishiya Naoyuki 岩手医科大学, 薬学部, 教授 (10286867)
• Co-Investigator(Kenkyū-buntansha): 大津 圭史 岩手医科大学, 歯学部, 准教授 (60509066)
• Project Period (FY): 2018-04-01 – 2021-03-31
• Keywords: mTOR / Wnt / 化合物 / 阻害薬

Outline of Final Research Achievements

ATP competitive kinase inhibitors have shown remarkable progress in the molecular targeting therapy for cancers. However, the identification of the new therapeutic target has been an important issue for the epoch-making drug discovery. We found that our Wnt/β-catenin signaling inhibitor (WSI) bound to a component of mTOR complex (mTORC), which is essential for mTORC functions. Therefore, we thought that pharmacological control of its function could become a new therapeutic strategy. In this study, we showed that WSI inhibited mTORC functions and controlled proliferation of cancer cells, and suggested usefulness of the component of mTORC as a new therapeutic target. This new target molecule may open up a next-generation drug discovery field.

Free Research Field

創薬科学

Academic Significance and Societal Importance of the Research Achievements

本研究は、画期的な新規創薬標的を提供するものであり、新たな創薬フロンティアを開拓する糸口となる。進行性腎細胞がんや神経内分泌腫瘍などのmTOR阻害薬が有効なアンメットメディカルニーズの高い疾患のための新たな治療選択の礎を築く。