Synthetic molecular approaches toward controlling intrinsically disordered proteins
| Project/Area Number |
18H02106
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Review Section |
Basic Section 37030:Chemical biology-related
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| Research Institution | Shinshu University |
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Principal Investigator |
Ohkanda Junko 信州大学, 学術研究院農学系, 教授 (50233052)
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| Project Period (FY) |
2018-04-01 – 2021-03-31
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| Project Status |
Completed (Fiscal Year 2020)
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| Budget Amount *help |
¥17,940,000 (Direct Cost: ¥13,800,000、Indirect Cost: ¥4,140,000)
Fiscal Year 2020: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Fiscal Year 2019: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Fiscal Year 2018: ¥13,520,000 (Direct Cost: ¥10,400,000、Indirect Cost: ¥3,120,000)
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| Keywords | 天然変性たんぱく質 / 脂質翻訳後修飾 / K-Ras / 概日時計転写因子 / リン酸化たんぱく質 / 14-3-3 / 中分子 / フシコクシン / 阻害剤 / KRas / 合理設計 / ライブラリ探索 / たんぱく質間相互作用 / K-Ras翻訳後修飾 / KRas脂質修飾阻害剤 / 14-3-3たんぱく質 / 非構造性たんぱく質 / IDPs |
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| Outline of Final Research Achievements |
Protein-protein interactions (PPIs) implicate in various diseases and intense efforts have focused on developing PPI-directed pharmaceuticals. However, structure-based drug design using drug-like small molecules still remains a difficult challenge due to the fact that the PPI interfaces that are often flat and flexible as seen in intrinsically disordered proteins (IDPs). Thus, a new methodology for designing and constructing synthetic agents that are capable of controlling intracellular PPIs that are reversible and transient. In this study, we elucidated three approaches based on synthetic molecules for controlling PPIs of intrinsically disordered proteins.
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| Academic Significance and Societal Importance of the Research Achievements |
たんぱく質間相互作用(PPI)創薬はポストゲノムの医療を拓く可能性が広く期待されている。また細胞応答などの過渡的な生命過程に関与する天然変性たんぱく質に対する化学的操作法への需要も高まっている。本研究の成果は、化合物による天然変性たんぱく質の機能調節の方法論を提案し、PPIの変調が関与するがんや神経変性疾患などの難病の治療薬開発を支える新しい創薬概念として役立つことが期待される。
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Report
(4 results)
Research Products
(44 results)
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[Journal Article] Structural Effects of Fusicoccin upon Upregulation of 14-3-3-Phospholigand Interaction and Cytotoxic Activity2018
Author(s)
Ohkanda Junko,Kusumoto Atsushi,Punzalan Louvy,Masuda Ryoma,Wang Chenyu,Parvatkar Prakash,Akase Dai,Aida Misako,Uesugi Motonari,Higuchi Yusuke,Kato Nobuo
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Journal Title
Chemistry - A European Journal
Volume: 24
Issue: 60
Pages: 16066-16071
DOI
Related Report
Peer Reviewed
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