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

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

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Detalles Bibliográficos
Autores principales: Asquith, Christopher R. M., Bennett, James M., Su, Lianyong, Laitinen, Tuomo, Elkins, Jonathan M., Pickett, Julie E., Wells, Carrow I., Li, Zengbiao, Willson, Timothy M., Zuercher, William J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6891286/
https://www.ncbi.nlm.nih.gov/pubmed/31698822
http://dx.doi.org/10.3390/molecules24224016