Challenges for the structure determination of GPCR active conformation
| Project/Area Number |
23657074
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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 |
Structural biochemistry
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| Research Institution | Kyoto University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
OGASAWARA Satoshi 京都大学, 医学研究科, 研究員 (30546685)
ASADA Hidetsugu 京都大学, 医学研究科, 研究員 (20399041)
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| Project Period (FY) |
2011 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2012: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2011: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Keywords | X線結晶解析 / 受容体 / GPCR / 膜タンパク質 / 構造解析 / G蛋白質共役型受容体 / X線結晶構造解析 |
|---|
| Research Abstract |
In order to understand the GPCR-mediated signal transduction mechanisms, it is essential to determine the GPCR structures in the active and inactive conformations. We published the structure of Histamine H1 receptor in complex with an inverse agonist doxepin. The structure revealed the reason why doxepin shows high affinities to aminergic receptors. We also published the structure of Adenosine A2a receptor in the inactive conformation. For crystallization, the receptor was stabilized in the inactive conformation by the binding of Fab fragment. The antibody that stabilizes the receptor in the active conformation was successfully obtained. This antibody will be useful for the determination of the Adenosine A2a receptor structure in the active conformation.
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Report
(3 results)
Research Products
(39 results)
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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(23)
Issue: 23
Pages: 8195-206
DOI
Related Report
Peer Reviewed
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[Journal Article] Structure ofthe human histamine H1 receptor complexwith doxepin.2011
Author(s)
Shimamura, T., Shiroishi, M, Weyand, S., Tsujimoto, H., Winter, G., Katritch, V., Abagyan, R., Cherezov, V., Liu, W., Han, G. W., Kobayashi, T., Stevens, R. C. and Iwata, S
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Journal Title
Nature
Volume: 475
Issue: 7354
Pages: 65-70
DOI
Related Report
Peer Reviewed
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[Journal Article] Cloning, expression and purification of the anion exchanger 1 homologue from the basidiomycete Phanerochaete chrysosporium2011
Author(s)
Tokuda N, Igarashi K, Shimamura T(co-1st author), 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(1)
Issue: 1
Pages: 81-7
DOI
NAID
Related Report
Peer Reviewed
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