2010 Fiscal Year Final Research Report
Design of DNA-cleaving and -crosslinking agents based on NFκB and HMGA proteins aiming at the application to cancer therapy
| Project/Area Number |
20390033
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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 Kumamoto University, 大学院・生命科学研究部, 教授 (40126008)
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| Co-Investigator(Kenkyū-buntansha) |
OKAMOTO Yoshinari 熊本大学, 大学院・生命科学研究部, 助教 (20194409)
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| Project Period (FY) |
2008 – 2010
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| Keywords | 癌 / NFκB / HMGA蛋白質 / DNA切断 |
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| Research Abstract |
Recently, NFκB and HMGA proteins attract the interest because of their relation to carcinogenesis and tumor invasion. The present study aimed at design and synthesis of DNA-cleaving/crosslinking molecules based on the NFκB and HMGA proteins.
We first synthesized a novel artificial ligand comprising a dimethylaminopyridine and histidines. This ligand formed ferrous complex to generate oxygen radical, cleaving DNA. In the present study, we are successful to prepare a new dimethylaminopyridine/histidine based ligand equipped with a chloroalkyl linker that could bind a SH group of various proteins in situ. This would enable us to cleave DNA sequences that NFκB and HMGA proteins recognize.
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[Journal Article] Properties and synthesis of 2-{2-Fluoro (or Bromo)-4-[(2-oxocyclopenty1)methyl]phenyl}propanoic acid : Non-steroidal Anti-inflammatory Drugs with Low Membrane Permeabilizing and Gastric Lesion-producing Activities.2010
Author(s)
Naoki Yamakawa, Shintaro Suemasu, Masaaki Matoyama, Ayumi Kimoto, Miho Takeda, Ken-ichiro Tanaka, Tomoaki Ishihara, Takashi Katsu, Yoshinari Okamoto, Masami Otsuka, Tohru Mizushima.
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Journal Title
J.Med.Chem. 53(21)
Pages: 7879-7882
Peer Reviewed
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[Journal Article] Identification of a New Series of STAT3 Inhibitors by Virtual Screening.2010
Author(s)
Kenji Matsuno, Yoshiaki Masuda, Yutaka Uehara, Hiroshi Sato, Ayumu Muroya, Osamu Takahashi, Takane Yokotagawa, Toshio Furuya, Tadashi Okawara, Masami Otsuka, Naohisa Ogo, Tadashi Ashizawa, Chie Oshita, Sachiko Tai, Hidee Ishii, Yasuto Akiyama, Akira Asai.
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Journal Title
ACS Med.Chem.Lett. 1(8)
Pages: 371-375
Peer Reviewed
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[Journal Article] Accerelated blood clearance phenomenon upon repeated injection of PEG-modified PLA-nanoparticles.2009
Author(s)
Tsutomu Ishihara, Miho Takeda, Haruka Sakamoto, Ayumi Kimoto, Chisa Kobayashi, Naoko Takasaki, Kanae Yuki, Ken-ichiro Tanaka, Mitsuko Takenaga, Rie Igarashi, Taishi Maeda, Naoki Yamakawa, Yoshinari Okamoto, Masami Otsuka, atsuhiro Ishida, Hiroshi Kiwada, Yutaka Mizushima, Tohru Mizushima.
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Journal Title
Pharmaceutical Research 26(10)
Pages: 2270-2279
Peer Reviewed
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[Journal Article] Synthesis of Prostaglandin E1 Phosphate Derivatives and Their Encapsulation in Biodegradable Nanoparticles.2009
Author(s)
Miho Takeda, Taishi Maeda, Tsutomu Ishihara, Haruka Sakamoto, Kanae Yuki, Naoko Takasaki, Fumihiro Nishimura, Takeshi Yamashita, Ken-ichiro Tanaka, Mitsuko Takenaga, Rie Igarashi, Megumu Higaki, Naoki Yamakawa, Yoshinari Okamoto, Hisao Ogawa, Masami Otsuka, Yutaka Mizushima, Tohru Mizushima.
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Journal Title
Pharmaceutical Research 26(7)
Pages: 1792-1800
Peer Reviewed
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