What is it about?
This paper describes two series of inhibitors of PI4-kinase that independently and selectively inhibit the α- and the β- isoforms with no significant activity towards related kinases in the pathway. In a cellular environment, inhibition of the α- but not the β- subtype led to a reduction in phosphatidylinositol-4-phosphate and phosphatidylinositol-4,5-phosphate concentration, causing inhibition of proliferation in a panel of cancer cell lines
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Why is it important?
These studies highlight the value of high quality small molecule inhibitors as probes to interpret complex biological cascades. The exquisite selectivity of the chemical probes allows their pharmacology to be ascribed to their intended targets with a high degree of confidence and should be of further utility in the study of PI4K biology and the PI pathway in general.
Read the Original
This page is a summary of: Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation, Chemical Communications, January 2014, Royal Society of Chemistry,
DOI: 10.1039/c3cc48391f.
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Accompanying slide set
Slides to accompany the paper. Presented by Mike Waring at the Chemical Biology Meets Drug Discovery Meeting - June 2014
2-Alkyloxazoles as potent and selective PI4KIIIβ inhibitors demonstrating inhibition of HCV replication
An interesting paper on the independent identification of an analogous series of compounds. Any similarities are serendipitous, the disease indication being virology rather than cancer.
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