A novel strategy to control of chemical transmission for transporter-targeted drug discovery
| Project/Area Number |
17K19489
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| Research Category |
Grant-in-Aid for Challenging Research (Exploratory)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Pharmaceutical Sciences and related fields
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| Research Institution | Okayama University |
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Principal Investigator |
Miyaji Takaaki 岡山大学, 自然生命科学研究支援センター, 研究教授 (40550314)
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| Project Period (FY) |
2017-06-30 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
Fiscal Year 2019: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2018: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2017: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
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| Keywords | トランスポーター / 化学伝達 / ATP / グルタミン酸 / 疼痛 / トランスポーター創薬 / 小胞型神経伝達物質トランスポーター |
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| Outline of Final Research Achievements |
Although neuropathic and inflammatory pain are unbearable chronic pain by various diseases, effective analgesics with few side effects have yet to be developed. In this study, we aimed to establish the control system of chemical transmission for transporter-targeted drug discovery. We identified several selective inhibitors of vesicular chemical transmitter transporter, which were more effective for chronic pain with few side effects than existing drugs. These compounds are expected to become new drug candidates for neuropathic and inflammatory pain.
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| Academic Significance and Societal Importance of the Research Achievements |
疼痛管理はQuality of Lifeの観点から重要であるが、副作用の少ない、効果的な鎮痛薬はこれまでにない。本研究により、化学伝達を司るトランスポーターの選択的阻害剤を同定し、既存の鎮痛薬よりも副作用なく、強力に鎮痛効果を発揮することを見出した。これら阻害剤は神経因性疼痛や炎症性疼痛の新しい創薬シーズになると期待される。
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Report
(4 results)
Research Products
(21 results)
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[Journal Article] Outward open conformation of a Major Facilitator Superfamily multidrug/H+ antiporter provides insights into switching mechanism2018
Author(s)
Nagarathinam K, Nakada-Nakura Y, Parthier C, Terada T, Juge N, Jaenecke F, Liu K, Hotta Y, Miyaji T, Omote H, Iwata S, Nomura N, Stubbs M, Tanabe M
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Journal Title
Nature Communications
Volume: 9
Issue: 1
Pages: 4005-4005
DOI
NAID
Related Report
Peer Reviewed / Open Access / Int'l Joint Research
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[Journal Article] Structural basis for xenobiotics extrusion by eukaryotic MATE transporter.2017
Author(s)
Miyauchi H., Moriyama S., Kusakizako T., Kumazaki K., Ito K., Dohmae N., Nishizawa T., Miyaji T., Moriyama Y., Ishitani R., Nureki O.
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Journal Title
Nature Commun.
Volume: 8
Issue: 1
Pages: 1633-1633
DOI
Related Report
Peer Reviewed / Open Access
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