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

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.

journal_name

Bioorg Med Chem Lett

authors

Raubo P,Andrews DM,McKelvie JC,Robb GR,Smith JM,Swarbrick ME,Waring MJ

doi

10.1016/j.bmcl.2015.05.093

subject

Has Abstract

pub_date

2015-08-15 00:00:00

pages

3189-93

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00576-4

journal_volume

25

pub_type

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