Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 3, Pages 340-345Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00399
Keywords
AAK1; BMP2K; acylaminoindazole; NAK family; endocytosis; protein kinase
Categories
Funding
- 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]
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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.
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