2017 Fiscal Year Final Research Report
Development of C1 domain ligand with selectivity for non-PKC type C1 domain-containing proteins
Project/Area Number |
15K18691
|
Research Category |
Grant-in-Aid for Young Scientists (B)
|
Allocation Type | Multi-year Fund |
Research Field |
Bioorganic chemistry
|
Research Institution | Kagawa University |
Principal Investigator |
|
Project Period (FY) |
2015-04-01 – 2018-03-31
|
Keywords | C1ドメイン / タプシガルギン / がん |
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.
|
Free Research Field |
農学
|