期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 3, 页码 340-345出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00399
关键词
AAK1; BMP2K; acylaminoindazole; NAK family; endocytosis; protein kinase
资金
- AbbVie
- Bayer Pharma AG
- Boehringer Ingelheim
- Canada Foundation for Innovation
- Eshelman Institute for Innovation
- Genome Canada
- Innovative Medicines Initiative (EU/EFPIA) [ULTRA-DD 115766]
- Janssen
- Merck KGaA Darmstadt Germany
- MSD
- Novartis Pharma AG
- Ontario Ministry of Economic Development and Innovation
- Pfizer
- Sao Paulo Research Foundation-FAPESP [2013/50724-5, 2014/50897-0, 2016/17469-0]
- Takeda
- Wellcome [106169/ZZ14/Z]
- Brazilian agency CNPq [465651/2014-3]
- NIH/NIGMS [GM083024, R25GM089569]
- HHMI Gilliam Fellowship for Advanced Study [GT10886]
- T32 award [T32GM007040]
- NC Biotech Center Institutional Support Grants [2017-IDG-1025, 2018-IDG-1030]
- NIH [1UM2AI30836-01]
- Spanish MECD [FPU 14/00818]
- [P30 CA016086]
- [1R44TR001916]
Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC-AAK1-1, 25) that is potent and selective for AAK1/BMP2K over other NAK family members, demonstrates narrow activity in a kinome-wide screen, and is functionally active in cells. This inhibitor represents one of the best available small molecule tools to study the functions of AAK1 and BMP2K.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据
分享论文
