Development of C1 domain ligand with selectivity for non-PKC type C1 domain-containing proteins
| Project/Area Number |
15K18691
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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 |
Bioorganic chemistry
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| Research Institution | Kagawa University |
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Principal Investigator |
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2017: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2016: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2015: ¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000)
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| Keywords | C1ドメイン / タプシガルギン / がん / セスキテルペンラクトン / アナログ設計 |
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| Outline of Final Research Achievements |
C1 domain is involved in 1,2-sn-diacylglycerol signaling and also bind natural tumor promoters including phorbol esters. We focused on thapsigargin (Tg), a sesquiterpene lactone isolated from Thapsia garganica, as a candidate for C1 domain ligand, and evaluated its affinity for C1 domains from various proteins. Tg exhibited little ability to bind to C1B domains of novel protein kinase C isozymes, main targets of natural tumor promoters, but exhibited substantial ability to bind to C1 domains of RasGRP4 and β-chimaerin. These results suggest the potential of Tg as a seed for C1 domain ligand with unique selectivity for subset of C1 domain-containing proteins such as RasGRP4 and β-chimaerin．
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Report
(4 results)
Research Products
(1 results)
