SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K

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-...

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Published inACS medicinal chemistry letters Vol. 11; no. 3; pp. 340 - 345
Main Authors Wells, Carrow, Couñago, Rafael M, Limas, Juanita C, Almeida, Tuanny L, Cook, Jeanette Gowen, Drewry, David H, Elkins, Jonathan M, Gileadi, Opher, Kapadia, Nirav R, Lorente-Macias, Alvaro, Pickett, Julie E, Riemen, Alexander, Ruela-de-Sousa, Roberta R, Willson, Timothy M, Zhang, Cunyu, Zuercher, William J, Zutshi, Reena, Axtman, Alison D
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 12.03.2020
Amer Chemical Soc
Subjects
Chemistry, Medicinal
Letter
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
AAK1
BMP2K
endocytosis
acylaminoindazole
NAK family
protein kinase
REGULATOR
INHIBITORS
ADAPTER-ASSOCIATED KINASE
IDENTIFICATION
FAMILY
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Summary: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.
Bibliography:FAPESP
ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.9b00399