Study of novel anti-leishmanial drug
Project/Area Number |
23659212
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Research Category |
Grant-in-Aid for Challenging Exploratory Research
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Allocation Type | Multi-year Fund |
Research Field |
Parasitology (including Sanitary zoology)
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Research Institution | Okayama University |
Principal Investigator |
WATAYA Yusuke 岡山大学, 大学院・医歯薬学総合研究科, 名誉教授 (90127598)
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Co-Investigator(Kenkyū-buntansha) |
KIM Hye-sook 岡山大学, 大学院・医歯薬学総合研究科, 准教授 (70314664)
SATO Akira 岡山大学, 大学院・医歯薬学総合研究科, 助教 (40530663)
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Project Period (FY) |
2011 – 2012
|
Project Status |
Completed (Fiscal Year 2012)
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Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2012: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
|
Keywords | リーシュマニア原虫 / アンチモン製剤 / 抗リーシュマニア活性評価 / Geldanamycin / Hsp90 / Leishmania major / Leishmania donovani / 天然生薬資源 / 感染症 / リーシュマニア / 創薬 / 難治性疾患 / 核酸誘導体 |
Research Abstract |
I performed to new drug discovery research for 68 compounds from organic compounds and natural product using promastigotes of Leishmania major. The EC50values among 2 of them for L. majorwere 42 nM and 27 nM. In contrast, Amphotericin B as a positive control was show 63 nM of EC50value for L. majorand selective toxicity of 46-fold compare tomammalian cells of it. The structure-activity relationship study will be need more. I established the mechanism analysis of HSP90 and complex relationship in L. major and also we found the high anti-leishmanial effect for HSP90 inhibitor and it’s analogs include small molecules (EC50values; 30-40 nM) against L. major promastigotes.
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Report
(3 results)
Research Products
(21 results)
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[Journal Article] Plasmodium falciparumendoplasmic reticulum-resident calcium binding protein is a possible target of synthetic antimalarial endoperoxides, N-89 and N-2512012
Author(s)
Morita, M., Sanai, H., Hiramoto, A., Sato, A., Hiraoka, O., Sakura, T., Kaneko, O., Masuyama, A., Nojima, M., Wataya, Y. and Kim, H.-S.
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Journal Title
J Proteome Res.
Volume: 11
Pages: 5704-11
URL
Related Report
Peer Reviewed
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[Journal Article] Andirolides HeP from the flower of andiroba (Carapa guianensis, Meliaceae)2012
Author(s)
Tanaka Y, Sakamoto A, Inoue T, Yamada T, Kikuchi T, Kajimoto T, Muraoka O, Sato A, Wataya Y, Kim H.-S, and Tanaka R.
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Journal Title
Tetrahedron
Volume: 68
Pages: 3669-77
URL
Related Report
Peer Reviewed
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[Journal Article] Plasmodium falciparum endoplasmic reticulum-resident calcium binding protein is a possible target of synthetic antimalarial endoperoxides, N-89 and N-2512012
Author(s)
Morita M., Sanai H., Hiramoto A., Sato A., Hiraoka O., Sakura T., Kaneko O., Masuyama A., Nojima M., Wataya Y., Kim H.-S.
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Journal Title
Journal of Proteome Research
Volume: 11
Issue: 12
Pages: 5704-5711
DOI
Related Report
Peer Reviewed
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[Journal Article] Andirolides H-P from the flower of andiroba (Carapa guianensis, Meliaceae)2012
Author(s)
Tanaka Y., Sakamoto A., Inoue T., Yamada T., Kikuchi T., Kajimoto T., Muraoka O., Sato A., Wataya Y., Kim H.-S., Tanaka R.
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Journal Title
Tetrahedron
Volume: 68
Issue: 18
Pages: 3669-3677
DOI
Related Report
Peer Reviewed
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[Journal Article] Antimalarial Activity of Endoperoxide Compound 6-(1,2,6,7- Tetraoxaspiro[7.11] nonadec-4-yl)hexan-1-ol.2011
Author(s)
Sato A., Hiramoto A., Morita M., Matsumoto M., Komich Y., Nakase Y., Tanigawa N., Hiraoka O., Hiramoto K., Hayatsu H., Higaki K., Kawai S., Masuyama A., Nojima M., Wataya Y., Kim H.-S.
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Journal Title
Parasitology International
Volume: 60
Pages: 270-3
URL
Related Report
Peer Reviewed
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[Journal Article] Schistosomicidal and antifecundity effects of oral treatment of synthetic endo-peroxide N-892011
Author(s)
Taniguchi T., Kumagai T., Shimogawara R., Ichinose S., Hiramoto A., Sato A., Morita M., Nojima M., Kim H.-S., Wataya Y., Ohta N.
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Journal Title
Parasitology International
Volume: 60
Pages: 231-6
URL
Related Report
Peer Reviewed
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[Journal Article] Antimalarial activity of 6-(1,2,6,7-tetraoxaspiro [7.11]nonadec-4-yl)hexan- 1-ol (N-251) and its carboxylic acid derivatives.2011
Author(s)
Sato A, Kawai S, Hiramoto A, Morita M, Tanigawa N, Nakase Y, Komichi Y, Matsumoto M, Hiraoka O, Hiramoto K, Tokuhara H, Masuyama A, Nojima M, Higaki K, Hayatsu H, Wataya Y, Kim HS.
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Journal Title
Parasitol. Int.
Volume: 60(4)
Pages: 488-92
URL
Related Report
Peer Reviewed
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[Journal Article] Antimalarial Activity of 6-(1,2,6,7-Tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251) and Its Carboxylic Acid Derivatives.2011
Author(s)
Sato A., Kawai S., Hiramoto A., Morita M., Tanigawa N., Nakase Y., Komichi Y., Matsumoto M., Hiraoka O., Hiramoto K., Tokuhara H., Masuyama A., Nojima M., Higaki K., Hayatsu H., et al.
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Journal Title
Parasitology International
Volume: 60
Pages: 488-492
Related Report
Peer Reviewed
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[Journal Article] Antimalarial Activity of Endoperoxide Compound 6-(1,2,6,7-Tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol.2011
Author(s)
Sato A., Hiramoto A., Morita M., Matsumoto M., Komichi Y., Nakase Y., Tanigawa N., Hiraoka O., Hiramoto K., Hayatsu H., Higaki K., Kawai S., Masuyama A., Nojima M., Wataya Y., Kim H.-S.
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Journal Title
Parasitology International
Volume: 60
Pages: 270-273
Related Report
Peer Reviewed
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[Journal Article] Schistosomicidal and antifecundity effects of oral treatment of synthetic endoperoxide N-89.2011
Author(s)
Taniguchi T., Kumagai T., Shimogawara R., Ichinose S., Hiramoto A., Sato A., Morita M., Nojima M., Kim H.-S., Wataya Y., Ohta N.
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Journal Title
Parasitology International
Volume: 60
Pages: 231-236
Related Report
Peer Reviewed
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[Presentation] Drug development research for antimalarial endoperoxide N-2512012
Author(s)
Masayuki Morita, Akiko Hiramoto, Kazuaki Okada, Tatsuya Wakimoto, Akane Katamoto, Hiroki Watanabe, Takuma Takahashi, Chikako Imada, Akira Sato, Kazutaka Higaki, Yusuke Wataya, Hye-Sook Kim
Organizer
Forum Cheju 15; The 15th Japan-Korea Parasitologists’ Seminar
Place of Presentation
Miyazaki, Japan
Related Report
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