Structural basis for auto-inhibition mechanisms of MAP2K
Project/Area Number |
15K07897
|
Research Category |
Grant-in-Aid for Scientific Research (C)
|
Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Physical pharmacy
|
Research Institution | Osaka Prefecture University |
Principal Investigator |
|
Project Period (FY) |
2015-04-01 – 2018-03-31
|
Project Status |
Completed (Fiscal Year 2017)
|
Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
|
Keywords | X線結晶構造解析 / キナーゼ / アロステリック阻害 / MAP2K / MAP2K7 / X線結晶構造解析 / 自己阻害機構 / 自己阻害構造 |
Outline of Final Research Achievements |
High resolution crystal structure was achieved by the protein stabilization and crystallization in the space and depicted two auto-inhibition mechanisms. (1) The n-σ* interaction of Cys218 with Gly145 occluded the ATP site. (2) The C-terminal extension bound to the N-terminal region of the adjacent molecules and worked as a negative regulator. A synthesized C-terminal region peptide moderately attenuated the enzyme activity.
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Report
(4 results)
Research Products
(18 results)