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Issue 40, 2014
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Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation

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Abstract

Two series of inhibitors of type III phosphatidylinositol-4-kinase were identified by high throughput screening and optimised to derive probe compounds 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-bisphosphate concentration, causing inhibition of inositol-1-phosphate formation and inhibition of proliferation in a panel of cancer cell lines.

Graphical abstract: Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation

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Publication details

The article was received on 01 Nov 2013, accepted on 12 Dec 2013 and first published on 13 Dec 2013


Article type: Communication
DOI: 10.1039/C3CC48391F
Author version available: Download Author version (PDF)
Citation: Chem. Commun., 2014,50, 5388-5390
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    Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation

    M. J. Waring, D. M. Andrews, P. F. Faulder, V. Flemington, J. C. McKelvie, S. Maman, M. Preston, P. Raubo, G. R. Robb, K. Roberts, R. Rowlinson, J. M. Smith, M. E. Swarbrick, I. Treinies, J. J. G. Winter and R. J. Wood, Chem. Commun., 2014, 50, 5388
    DOI: 10.1039/C3CC48391F

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