2012 Fiscal Year Final Research Report
Structural basis for the drug binding of human alpha1-acid glycoprotein
| Project/Area Number |
23790052
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Physical pharmacy
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| Research Institution | Kumamoto University |
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Principal Investigator |
NAKAMURA Teruya 熊本大学, 大学院・生命科学研究部, 助教 (40433015)
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| Project Period (FY) |
2011 – 2012
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| Keywords | 薬物結合蛋白質 / 構造活性相関 / X線結晶構造解析 |
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| Research Abstract |
Human a1-acid glycoprotein binds to a variety of drugs and therebyregulates their tissue distribution. AGP exists as a mixture of two genetic variants,the A and F1*S variants, which bind drugs with different selectivities. In this study,we determined crystal structures of the A variant in complex with two types of tricyclicdrugs, and revealed their binding modes in the pocket of the A variant. Also, we mutatedthe amino acid residues which are involved in drug binding, and examined the bindingproperties of the mutants.
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[Journal Article] Crystallization and preliminary X-rayanalysis of human MTH1 with a homogeneousN-terminus2013
Author(s)
Koga, Y., Inazato, M., Nakamura, T.,Hashikawa, C., Chirifu, M., Michi, A.,Yamashita, T., Toma, S., Kuniyasu, A.,Ikemizu, S., Nakabeppu, Y., Yamagata, Y.
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Journal Title
Acta Cryst
Volume: F69
Pages: 45-48
DOI
Peer Reviewed
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[Journal Article] Diverse substraterecognition and hydrolysis mechanisms ofhuman NUDT52011
Author(s)
Arimori, T., Tamaoki, H., Nakamura, T.,Kamiya, H., Ikemizu, S, Takagi, Y,Ishibashi, T, Harashima, H, Sekiguchi, M,Yamagata, Y.
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Journal Title
Nucleic Acids Res.
Volume: 39
Pages: 8972-8983
DOI
Peer Reviewed
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[Journal Article] Structural insightsinto differences in drug bindingselectivity between two forms of humanalfa1-acid glycoprotein genetic variants,the A and F1*S forms.2011
Author(s)
Nishi, K., Ono, T., Nakamura, T.,Fukunaga, N., Izumi, M., Watanabe, H.,Suenaga, A., Maruyama, T., Yamagata, Y.,Curry, S., Otagiri, M.
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Journal Title
J. Biol. Chem.
Volume: 286
Pages: 14427-34
DOI
Peer Reviewed
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