2022 Fiscal Year Final Research Report
Development of new anti-cancer drug with anti-apoptotic protein MCL-1 selective inhibitory activity
| Project/Area Number |
20K06977
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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| Research Institution | Meiji Pharmaceutical University |
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Principal Investigator |
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| Project Period (FY) |
2020-04-01 – 2023-03-31
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| Keywords | 海洋天然物 / 抗がん剤 / イソキノリンアルカロイド / アポトーシス / Mcl-1 / がん幹細胞 |
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| Outline of Final Research Achievements |
Lung cancer is the most prevalent cause of cancer death, and according to estimates of the global cancer statistics of incidence and mortality of all types of malignancies, its incidence is increasing. Derivatives of the RT right-half analog were used to treat NSCLC cells (H460 and H23) to analyze cell viability. The results revealed that the right half model compound of RT with thiazole ring, named DH-25, shows very potent anticancer activity against NSCLC. The compound was also shown to be effective against cancer stem cells, which have been implicated in cancer recurrence and drug resistance.
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| Free Research Field |
天然物化学、医薬品化学
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| Academic Significance and Societal Importance of the Research Achievements |
本邦において死因のトップであるがんを新しい作用で治療する医薬品の開発をおこなった。がんの根治が難しい要因として、がん細胞が医薬品に対し抵抗性を示すことが挙げられる。我々が開発した化合物は、この抵抗性に関与しているタンパク質を減少させることで、がん細胞自らを細胞死（アポトーシス）させることができる。
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