2012 Fiscal Year Final Research Report
Elucidation of physiological role of the fatty acid receptor bycomputer simulation and the fluorescent probe detection system
| Project/Area Number |
23659038
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Biological pharmacy
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| Research Institution | Kyoto University |
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Principal Investigator |
HIRASAWA Akira 京都大学, 大学院・薬学研究科, 准教授 (70242633)
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| Co-Investigator(Renkei-kenkyūsha) |
LIU Ning 京都大学, 大学院・薬学研究科, 研究員 (70464196)
IIDA Keiko 京都大学, 大学院・薬学研究科, 教務補佐 (00422999)
AWAJI Takeo 埼玉医科大学, 医学部, 講師 (60297546)
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| Project Period (FY) |
2011 – 2012
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| Keywords | 分子生物学脂肪酸受容体 / GPR40 / GPR120 / 蛍光プローブ / 肥満 / シミュレーション |
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| Research Abstract |
The free fatty acid GPR40 receptor and GPR120 are GPCRs whose endogenous ligands are medium- and long-chain FFAs, and they are important in regulating insulin and GLP-1 secretion respectively.T o clarify the mechanism of diet-induced obesity caused by GPR120 defect, we performed physiological, expression profile and lipidomics analysis and developed a mathematical model. We succeeded to find the compound with the highest predicted selectivity for GPR40 receptors from this structure-activity relationship analysis.Furthermore, we analyzed in more detail physiology GPR120 with a fluorescentprobe in order to detect a direct interaction of the receptor. We revealed that the lipid sensor GPR120 is involved in obesity in both mice and humans.A large contribution to drug development using this study results is expected
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Research Products
(10 results)
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[Journal Article] Structure-Based Design of Novel Potent Protein Kinase CK2 (CK2) Inhibitors with Phenyl-azole Scaffolds2012
Author(s)
Hou Z, Nakanishi I, Kinoshita T, Takei Y, Yasue M, Misu R, Suzuki Y, Nakamura S, Kure T, Ohno H, Murata K, Kitaura K, Hirasawa A, Tsujimoto G, Oishi S, Fujii N
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Journal Title
J Med Chem
Volume: 55
Pages: 2899-2903
Peer Reviewed
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[Journal Article] Paradoxical Downregulation of CXC Chemokine Receptor 4 Induced by Polyphemusin II-derived Antagonists.2012
Author(s)
Masuda R, Oishi S, Tanahara N, Ohno H, Hirasawa A, Tsujimoto G, Yano Y, Matsuzaki K, Navenot J M, Peiper S C, Fujii N
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Journal Title
Peer Reviewed
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[Journal Article] Design and synthesis of a novel class of CK2 inhibitors: application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles.2012
Author(s)
Suzuki Y, Oishi S, Takei Y, Yasue M, Misu R, Naoe S, Hou Z, Kure T, Nakanishi I, Ohno H, Hirasawa A, Tsujimoto G, Fujii N
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Journal Title
Org Biomol Chem
Volume: 10
Pages: 4907-4915
Peer Reviewed
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