Development of lamellarin type axially chiral molecules aiming at the creation of selective kinase inhibitors
Project/Area Number |
15K01802
|
Research Category |
Grant-in-Aid for Scientific Research (C)
|
Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Biomolecular chemistry
|
Research Institution | Nagasaki University |
Principal Investigator |
|
Co-Investigator(Renkei-kenkyūsha) |
SHIGEMITSU Yasuhiro 長崎大学, 工学研究科, 准教授 (50432969)
|
Project Period (FY) |
2015-04-01 – 2018-03-31
|
Project Status |
Completed (Fiscal Year 2017)
|
Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2015: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
|
Keywords | ラメラリン / 軸不斉 / アトロプ異性体 / プロテインキナーゼ / ハロゲン化 |
Outline of Final Research Achievements |
Axially chiral 16-chloro and 16-bromolamellarins N have been developed for the creation of selective kinase inhibitors. The kinase inhibitory activities of these enantiomers were evaluated on seven protein kinases. The (aR)-isomers of 16-chloro and 16-bromolamellarins N exhibited potent but non-selective inhibition on five protein kinases except for CK1ε and CLK3. On the other hand, the (aS)-isomers showed selective inhibition against only DYRK1A, GSK-3β, and PIM1.
|
Report
(4 results)
Research Products
(25 results)
-
-
[Journal Article] Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant2017
Author(s)
Tsutomu Fukuda, Teppei Umeki, Keiji Tokushima, Gao Xiang, Yuki Yoshida, Fumito Ishibashi, Yusuke Oku, Naoyuki Nishiya, Yoshimasa Uehara, Masatomo Iwao
-
Journal Title
Bioorganic & Medicinal Chemistry
Volume: 25
Issue: 24
Pages: 6563-6580
DOI
NAID
Related Report
Peer Reviewed / Open Access / Int'l Joint Research
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-