Development of artificial antibody of anti-bitter taste receptor using random amino acid sequence library
| Project/Area Number |
16K08426
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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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| Research Field |
Medical pharmacy
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| Research Institution | Mukogawa Women's University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
吉田 都 武庫川女子大学, 薬学部, 准教授 (20369028)
伊東 祐二 鹿児島大学, 理工学域理学系, 教授 (60223195)
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| Project Period (FY) |
2016-04-01 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2019: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2018: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2017: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2016: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 味覚センサ / Asp-Asp / Glu-Glu / アスパラギン酸 / グルタミン酸 / hTAS2R14 / 表面プラズモン共鳴 / 分子モデリング / 分子モデルシュミレーション / 疎水性相互作用 / 静電相互作用 / ミセル / SPR / Asp / Glu / ペプチド / アミノ酸 / ヒト苦味受容体 / Glu-Asp / ジフェンヒドラミン塩酸塩 / ドネペジル塩酸塩 / アムロジピンベシル酸塩 / 医療薬剤学 |
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| Outline of Final Research Achievements |
We firstly found the correlation between taste sensor output of commercial medicines and their response in various type of human receptors. Secondly, the inhibition of Asp-Asp and Glu-Glu as umami-peptides and their constituent Asp and Glu as amino acid toward 0.5 mM diphenhydramine hydrochloride (DPH) solution were examined. The Asp-Asp and Glu-Glu dramatically reduced bitterness sensor output of DPH in their concentration dependent manner. In the SPR experiment, the spectrum change was ranked as follows: Asp-Asp>Glu-Glu>Asp>Glu. This information and docking simulation study suggested that competitive inhibition of umami-peptide via binding to binding site of hTAS2R14
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| Academic Significance and Societal Importance of the Research Achievements |
苦味を呈する医薬品は苦味受容体タンパク(hTAS2R10、hTAS2R14他)の基質であることが確認されているが特異的な苦味抑制剤は開発されていない。研究代表者は多くのペプチド、アミノ酸類の中から旨味ペプチドに着目し、塩基性薬物への有意な苦味抑制効果を味覚センサで検証し、その機序について表面プラズモン共鳴 (SPR）と分子モデリングにより予測した。検討により多くの塩基性薬物について比較的低分子のAsp-Asp、Glu-GluならびにAsp、Gluが一定の苦味抑制効果を示すことを見出した点に本研究の意義がある。今後分子モデリングの活用により苦味受容体のインバースアゴニストの分子設計に応用できる。
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Report
(5 results)
Research Products
(17 results)
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[Journal Article] Bitterness-Suppressing Effect of Umami Dipeptides and Their Constituent Amino Acids on Diphenhydramine: Evaluation by Gustatory Sensation and Taste Sensor Testing2020
Author(s)
Takayoshi Okuno, Shiori Morimoto, Haruka Nishikawa, Tamami Haraguchi, Honami Kojima, Hirofumi Tsujino, Mitsuhiro Arisawa, Taku Yamashita, Junichi Nishikawa, Miyako Yoshida, Masaaki Habara, Hidekazu Ikezaki, Takahiro Uchida
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Journal Title
Chemical and Pharmaceutical Bulletin
Volume: 68
Issue: 3
Pages: 234-243
DOI
NAID
ISSN
0009-2363, 1347-5223
Year and Date
2020-03-01
Related Report
Peer Reviewed / Open Access
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[Journal Article] Bitterness-Masking Effects of Different Beverages on Zopiclone and Eszopiclone Tablets2019
Author(s)
Yoshida M., Kojima H., Uda A., Haraguchi T., Ozeki M., Kawasaki I., Yamamoto K., Yano I., Hirai M., Uchida T.
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Journal Title
Chemical and Pharmaceutical Bulletin
Volume: 67
Issue: 5
Pages: 404-409
DOI
NAID
ISSN
0009-2363, 1347-5223
Year and Date
2019-05-01
Related Report
Peer Reviewed / Open Access
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