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High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds

   
@article{APS9881,
	author = {Jia Wang and Grace Qun Gong and Yan Zhou and Woo-Jeong Lee and Christina Maree Buchanan and William Alexander Denny and Gordon William Rewcastle and Jackie Diane Kendall and James Michael Jeremy Dickson and Jack Urquhart Flanagan and Peter Robin Shepherd and De-Hua Yang and Ming-Wei Wang},
	title = {High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds},
	journal = {Acta Pharmacologica Sinica},
	volume = {39},
	number = {11},
	year = {2018},
	keywords = {},
	abstract = {The phosphatidylinositol 3-kinase (PI3K) pathway is involved in many cellular functions including cell growth, metabolism, and transformation. Hyperactivation of this pathway contributes to tumorigenesis, therefore, PI3K is a major target for anticancer drug discovery. Since the PI3Kα isoform is implicated mostly in cancer, we conducted a high-throughput screening (HTS) campaign using a 3-step PI3K homogenous time-resolved fluorescence assay against this isoform bearing the H1047R mutation. A total of 288,000 synthetic and natural product-derived compounds were screened and of which, we identified 124 initial hits that were further selected by considering the predicted binding mode, relationship to known pan-assay interference compounds and previous descriptions as a lipid kinase inhibitor. A total of 24 compounds were then tested for concentration-dependent responses. These hit compounds provide novel scaffolds that can potentially be optimized to create novel PI3K inhibitors.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/9881}
}