2012 Fiscal Year Final Research Report
Elucidating of inhibition mechanism of anti-histamines for the histamine receptor by X-ray crystallography.
| Project/Area Number |
23770123
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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 |
Structural biochemistry
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| Research Institution | Kyushu University |
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Principal Investigator |
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| Project Period (FY) |
2011 – 2012
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| Keywords | G蛋白質共役型受容体 / 結晶構造解析 / 機能解析 |
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| Research Abstract |
We developed a platform using budding yeast (S. crevisiae) and green fluorescent protein (GFP) for the rapid construction and evaluation of GPCR variants for structural studies. This platform cut the process time in one third. We produced a stable and highly-expressed histamine H1 receptor (H1R) using this platform. We determined the crystal structure of the H1R in complex with doxepin, an inverse agonist antihistamine. The H1R structure provides key information that should aid the development of highly selective antihistamines.
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Research Products
(17 results)
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[Journal Article] Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist.2012
Author(s)
Haga K, Kruse AC, Asada H, Yurugi-Kobayashi T, Shiroishi M, Zhang C, Weis WI, Okada T, Kobilka BK, Haga T, Kobayashi T
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Journal Title
Nature
Volume: 482
Pages: 547-551
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[Journal Article] Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.2011
Author(s)
de Graaf C, Kooistra AJ, Vischer HF, Katritch V, Kuijer M, Shiroishi M, Iwata S, Shimamura T, Stevens RC, de Esch IJ, Leurs R.
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Journal Title
J Med Chem.
Volume: 54
Pages: 8195-8206
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[Journal Article] Structure of the human histamine H(1) receptor complex with doxepin.2011
Author(s)
Shimamura T*, Shiroishi M*, Weyand S, Tsujimoto H, Winter G, Katritch V, Abagyan R, Cherezov V, Liu W, Han GW, Kobayashi T, Stevens RC, Iwata S.
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Journal Title
Nature
Volume: 475
Pages: 65-70
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[Journal Article] Cloning, expression and purification of the anion exchanger 1 homologue from the basidiomycete Phanerochaete chrysosporium.2011
Author(s)
Tokuda N, Igarashi K, Shimamura T, Yurugi-Kobayashi T, Shiroishi M, Ito K, Sugawara T, Asada H, Murata T, Nomura N, Iwata S, Kobayashi T.
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Journal Title
Protein Expr Purif.
Volume: 79
Pages: 81-87
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[Journal Article] Evaluation of the Pichia pastoris expression system for the production of GPCRs for structural analysis.2011
Author(s)
Asada H, Uemura T, Yurugi-Kobayashi T, Shiroishi M, Shimamura T, Tsujimoto H, Ito K, Sugawara T, Nakane T, Nomura N, Murata T, Haga T, Iwata S, Kobayashi T.
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Journal Title
Microb Cell Fact.
Pages: 10-24
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