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Type: Artigo
Title: SGC-AAK1-1: A chemical probe targeting AAK1 and BMP2K
Author: Wells, C.
Couñago, R.M.
Limas, J.C.
Almeida, T.L.
Cook, J.G.
Drewry, D.H.
Elkins, J.M.
Gileadi, O.
Kapadia, N.R.
Lorente-Macias, A.
Pickett, J.E.
Riemen, A.
Ruela-De-Sousa, R.R.
Willson, T.M.
Zhang, C.
Zuercher, W.J.
Zutshi, R.
Axtman, A.D.
Abstract: 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
Subject: Sulfonas
Country: Estados Unidos
Editor: American Chemical Society
Rights: Fechado
Identifier DOI: 10.1021/acsmedchemlett.9b00399
Date Issue: 2020
Appears in Collections:IB - Artigos e Outros Documentos
CBMEG - Artigos e Outros Documentos

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