2013 Fiscal Year Final Research Report
Chemical control of protein dramatype
| Project/Area Number |
22249006
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| Research Category |
Grant-in-Aid for Scientific Research (A)
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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 | The University of Tokyo |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
ISHIKAWA Minoru 東京大学, 分子細胞生物学研究所, 准教授 (70526839)
AOYAMA Hiroshi 東京大学, 分子細胞生物学研究所, 助教 (40374699)
SUGITA Kazuyuki 東京大学, 分子細胞生物学研究所, 准教授 (60542090)
KOBAYASHI Hisayoshi 東京大学, 分子細胞生物学研究所, 助教 (80225531)
YACHIDE Tomomi 東京大学, 分子細胞生物学研究所, 技術職員 (20401284)
MATSUMOTO Yotaro 東京大学, 分子細胞生物学研究所, 助教 (90420041)
MISAWA Takashi 東京大学, 分子細胞生物学研究所, 助教 (40709820)
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| Project Period (FY) |
2010-04-01 – 2014-03-31
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| Keywords | トラフィッキング / フォールディング異常症 / 蛋白変性症 / マルチテンプレート / 核内受容体リガンド / 生理活性物質 / 蛋白質相互作用 / 膜タンパク質 |
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| Research Abstract |
Function, expression, stability and cellular localization of proteins are determined by their three dimensional structure. Therefore, control of the conformation of proteins results on regulation of their function/stability/localization. Abnormal conformation of specific proteins results in various incurable diseases. This research projects resulted in creation of: (1) various nuclear receptor ligands which control the function of the receptors by regulating their conformation, (2) small molecules (pharmacological chaperons) which correct abnormal trafficking of mutated proteins (ex. mutated rhodopsin which causes retinitis pigmentosa, NPC1 which caused Niemann-Pick type 1 disease), and (3) small molecules (SNIPERS) which induce degradation of target proteins in living cells.
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Research Products
(35 results)
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[Journal Article] Design, synthesis, and biological evaluation of novel trans repression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6 H-dibenz[b,e]azepin-6-one skeleton2012
Author(s)
A.Aoyama, K.Endo-Umeda, K.Kishida, K.Ohgane, T.Noguchi-Yachide, H.Aoyama, M.Ishikawa, H.Miyachi, M.Makishima, Y.Hashimoto
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Journal Title
J. Med. Chem.
Volume: 55
Pages: 7360-7377
DOI
Peer Reviewed
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