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From PIM1 to PI3Kδ via GSK3β: Target hopping through the kinome

Henley, Zoë A., Bax, Benjamin D., Inglesby, Laura M., Champigny, Aurélie, Gaines, Simon, Faulder, Paul, Le, Joelle, Thomas, Daniel A., Washio, Yoshiaki and Baldwin, Ian R. 2017. From PIM1 to PI3Kδ via GSK3β: Target hopping through the kinome. ACS Medicinal Chemistry Letters 8 (10) , pp. 1093-1098. 10.1021/acsmedchemlett.7b00296

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Selective inhibitors of phosphoinositide 3-kinase delta are of interest for the treatment of inflammatory diseases. Initial optimization of a 3-substituted indazole hit compound targeting the kinase PIM1 focused on improving selectivity over GSK3β through consideration of differences in the ATP binding pockets. Continued kinase cross-screening showed PI3Kδ activity in a series of 4,6-disubstituted indazole compounds, and subsequent structure–activity relationship exploration led to the discovery of an indole-containing lead compound as a potent PI3Kδ inhibitor with selectivity over the other PI3K isoforms.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Biosciences
Publisher: American Chemical Society
ISSN: 1948-5875
Date of First Compliant Deposit: 8 May 2018
Date of Acceptance: 5 September 2017
Last Modified: 10 May 2018 06:30

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