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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.

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.
AuthorsMichael J Waring, David M Andrews, Paul F Faulder, Vikki Flemington, Jennifer C McKelvie, Sarita Maman, Marian Preston, Piotr Raubo, Graeme R Robb, Karen Roberts, Rachel Rowlinson, James M Smith, Martin E Swarbrick, Iris Treinies, Jon J G Winter, Robert J Wood
JournalChemical communications (Cambridge, England) (Chem Commun (Camb)) Vol. 50 Issue 40 Pg. 5388-90 (May 25 2014) ISSN: 1364-548X [Electronic] England
PMID24366037 (Publication Type: Journal Article)
Chemical References
  • Inositol Phosphates
  • Phosphatidylinositol 4,5-Diphosphate
  • Phosphatidylinositol Phosphates
  • Protein Kinase Inhibitors
  • Small Molecule Libraries
  • phosphatidylinositol 4-phosphate
  • inositol 1-phosphate
  • 1-Phosphatidylinositol 4-Kinase
Topics
  • 1-Phosphatidylinositol 4-Kinase (antagonists & inhibitors)
  • Cell Proliferation (drug effects)
  • High-Throughput Screening Assays
  • Humans
  • Inositol Phosphates (antagonists & inhibitors, metabolism)
  • Models, Molecular
  • Molecular Structure
  • Neoplasms (drug therapy, metabolism, pathology)
  • Phosphatidylinositol 4,5-Diphosphate (metabolism)
  • Phosphatidylinositol Phosphates (metabolism)
  • Protein Kinase Inhibitors (pharmacology)
  • Signal Transduction (drug effects)
  • Small Molecule Libraries (pharmacology)
  • Tumor Cells, Cultured

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