2012 Fiscal Year Final Research Report
Structure‐activity relationship studies of CYP2C9 genetic variants
| Project/Area Number |
22590054
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Physical pharmacy
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| Research Institution | National Institute of Health Sciences |
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Principal Investigator |
MAEKAWA Keiko 国立医薬品食品衛生研究所, 医薬安全科学部, 室長 (70270626)
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| Co-Investigator(Kenkyū-buntansha) |
SAITO Yoshiro 国立医薬品食品衛生研究所, 医薬安全科学部, 部長 (50215571)
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| Co-Investigator(Renkei-kenkyūsha) |
ADACHI Motoyasu 独立行政法人日本原子力研究開発機構, 量子ビーム応用研究部門, 研究副主幹 (60293958)
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| Project Period (FY) |
2010 – 2012
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| Keywords | 構造生物学 |
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| Research Abstract |
To evaluate structure‐activity relationship of CYP2C9 genetic variants, CYP2C9*3, CYP2C9*28, CYP2C9*30, found in Japanese, in vitro functional study and X-ray crystallography were performed using recombinant CYP2C9 enzymes. Two variants, CYP2C9.3 and CYP2C9.30 showed decreased catalytic activities toward glyburide. X-ray crystallography revealed that amino acid substitution by CYP2C9*30 might influence the binding of losartan at substrate binding site.
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