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Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα)

Lookup NU author(s): Professor Mike Waring

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Abstract

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.

Publication metadata

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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