Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK)

Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK)

SGC-GAK-1 (<b>1</b>) is a potent, selective, cell-active chemical probe for cyclin G-associated kinase (GAK). However, <b>1</b> was rapidly metabolized in mouse liver microsomes by cytochrome P450-mediated oxidation, displaying rapid clearance in liver microsomes and in mice,...

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Bibliographic Details
Main Authors: Christopher R. M. Asquith, James M. Bennett, Lianyong Su, Tuomo Laitinen, Jonathan M. Elkins, Julie E. Pickett, Carrow I. Wells, Zengbiao Li, Timothy M. Willson, William J. Zuercher
Format: Article
Language:English
Published: MDPI AG 2019-11-01
Series:Molecules
Subjects:
cyclin g associated kinase (gak)
kinase inhibitor design
in vivo kinase design
1-aminobenzotriazole (abt)
Online Access:https://www.mdpi.com/1420-3049/24/22/4016

Internet

https://www.mdpi.com/1420-3049/24/22/4016

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