A new concept for drug discovery from peptide natural products
Project/Area Number |
24659004
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Research Category |
Grant-in-Aid for Challenging Exploratory Research
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Allocation Type | Multi-year Fund |
Research Field |
Chemical pharmacy
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Research Institution | Kyoto University |
Principal Investigator |
OISHI Shinya 京都大学, 薬学研究科(研究院), 講師 (80381739)
|
Project Period (FY) |
2012-04-01 – 2015-03-31
|
Project Status |
Completed (Fiscal Year 2014)
|
Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2013: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
|
Keywords | ペプチド / 二次代謝産物 / 天然物 / 全合成 / 薬らしさ |
Outline of Final Research Achievements |
Facile synthetic approaches to peptide natural products with multiple N-methyl amide bonds were investigated. For the synthesis of antiproliferative coibamide A, the solid-phase protocols were optimized. The macrolactonization of the linear precursor provided a coibamide A epimer with slightly less potent antiproliferative activity. Additionally, a facile synthetic process of IB-01212 via multiple N-methylation was established. The structure-activity relationship of a series of the derivatives revealed that the peptide conformation would mainly contribute to the bioactivity.
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Report
(4 results)
Research Products
(22 results)
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[Presentation] Synthetic Studies on Coibamide A
Author(s)
Ryota Nabika, Shinya Oishi, Hiroaki Ohno, Nobutaka Fujii
Organizer
The First Asian Conference for ''MONODUKURI'' Strategy by Synthetic Organic Chemistry
Place of Presentation
Southern Beach Hotel & Resort Okinawa(沖縄県糸満市)
Related Report
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