2013 Fiscal Year Final Research Report
Development of medicinal molecules having biologically functions targeting the PI3K/Akt pathway and the TGF-b/Smad pathway
| Project/Area Number |
23390028
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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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| Research Field |
Drug development chemistry
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| Research Institution | Kumamoto University |
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Principal Investigator |
OTSUKA Masami 熊本大学, 大学院生命科学研究部(薬), 教授 (40126008)
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| Co-Investigator(Renkei-kenkyūsha) |
FUJITA Mikako 熊本大学, 薬学部, 准教授 (00322256)
OKAMOTO Yoshinari 熊本大学, 大学院・生命科学研究部, 助教 (20194409)
ANRAKU Kensaku 熊本保健科学大学, 保健科学部, 講師 (80389543)
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| Project Period (FY) |
2011-04-01 – 2014-03-31
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| Keywords | ＰＩ３Ｋ／Ａｋｔ経路 / ＴＧＦ‐β／Ｓｍａｄ経路 / 脳保護 / 癌 / 強皮症 |
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| Research Abstract |
The present study aimed at the design and synthesis of activators of the PI3K/Akt pathway and inhibitors of the TGF-b/Smad pathway to develop drugs to regulate the crosstalk of the two pathways. Targeting the PI3K/Akt pathway, compounds comprising inositol phosphate and diacyl glycerol moiety were synthesized. Targeting the TGF-b/Smad pathway, compounds comprising the pyridine and metal-binding side chains were synthesized. These compounds could be useful as brain-protecting agents, drugs for diabetes, cancer, cancer metastasis, and scleroderma.
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[Journal Article] Design and synthesis of lipid-coupled inositol 1, 2, 3, 4, 5, 6-hexakisphosphate derivatives exhibiting high-affinity binding for HIV-1 MA domain2014
Author(s)
Hiroshi Tateishi, Kensaku Anraku, Ryoko Koga, Yoshinari Okamoto, Mikako Fujita, Masami Otsuka
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Journal Title
Organic & Biomolecular Chemistry
Volume: (First published online)
DOI
Peer Reviewed
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[Journal Article] Poly-proline motif in HIV-2 Vpx is critical for its efficient translation2014
Author(s)
Ariko Miyake, Mikako Fujita, Haruna Fujino, Ryoko Koga, Sogo Kawamura, Masami Otsuka, Hirotaka Ode, Yasumasa Iwatani, Yosuke Sakai, Naoya Doi, Masako Nomaguchi, Akio Adachi, Yasuyuki Miyazaki
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Journal Title
Journal of General Virology
Volume: 95
Pages: 179-189
DOI
Peer Reviewed
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[Journal Article] Effect of the STAT3 inhibitor STX-0119 on the proliferation of cancer stem-like cells derived from recurrent glioblastoma2013
Author(s)
Tadashi Ashizawa, Haruo Miyata, Akira Iizuka, Masaru Komiyama, Chie Oshita, Akiko Kume, Masahiro Nogami, Mika Yagoto, Ichiro Ito, Takuma Oishi, Reiko Watanabe, Koichi Mitsuya, Kenji Matsuno, Toshio Furuya, Tadashi Okawara, Masami Otsuka, Naohisa Ogo, Akira Asai, Yoko Nakasu, Ken Yamaguchi Yasuto Akiyama
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Journal Title
International Journal of Oncology
Pages: 219-227
DOI
Peer Reviewed
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[Journal Article] Identification of a unique nsaid, fluoro-loxoprofen with gastroprotective activity2012
Author(s)
Shintaro Suemasu, Naoki Yamakawa, Tomoaki Ishihara, Teita Asano, Kayoko Tahara, Ken-ichiro Tanaka, Hirofumi Matsui, Yoshinari Okamoto, Masami Otsuka, Koji Takeuchi, Hidekatsu Suzuki, Tohru Mizushima
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Journal Title
Biochemical Pharmacology
Volume: 84(11)
Pages: 1470-1481
DOI
Peer Reviewed
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[Journal Article] Design and synthesis of biotinylated inositol 1, 3, 4, 5-tetrakisphosphate targeting Grp1 Pleckstrin Homogy domain2011
Author(s)
Kensaku Anraku, Teruhiko Inoue, Kenji Sugimoto, Kota Kudo, Yoshinari Okamoto, Takashi Morii, Yasuo Mori, Masami Otsuka
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Journal Title
Bioorg. Med. Chem
Volume: 19(22)
Pages: 6833-6841
DOI
Peer Reviewed
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