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Lookup NU author(s): Professor Mike Waring
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The discovery and optimisation of novel, potent and selective small molecule inhibitors of the α-isoform of type III phosphatidylinositol-4-kinase (PI4Kα) are described. Lead compounds show cellular activity consistent with their PI4Kα potency inhibiting the accumulation of IP1 after PDGF stimulation and reducing cellular PIP, PIP2 and PIP3 levels. Hence, these compounds are useful in vitro tools to delineate the complex biological pathways involved in signalling through PI4Kα.
Author(s): Raubo P, Andrews DM, McKelvie JC, Robb GR, Smith JM, Swarbirck ME, Waring MJ
Publication type: Article
Publication status: Published
Journal: Bioorganic & Medicinal Chemistry Letters
Year: 2015
Volume: 25
Issue: 16
Pages: 3189-3193
Print publication date: 15/08/2015
Online publication date: 04/06/2015
Acceptance date: 29/05/2015
ISSN (print): 0960-894X
ISSN (electronic): 1464-3405
Publisher: Pergamon Press
URL: http://dx.doi.org/10.1016/j.bmcl.2015.05.093
DOI: 10.1016/j.bmcl.2015.05.093
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