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High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.
Wang J, Gong GQ, Zhou Y, Lee WJ, Buchanan CM, Denny WA, Rewcastle GW, Kendall JD, Dickson JMJ, Flanagan JU, Shepherd PR, Yang DH, Wang MW. Wang J, et al. Among authors: shepherd pr. Acta Pharmacol Sin. 2018 Nov;39(11):1816-1822. doi: 10.1038/s41401-018-0057-z. Epub 2018 Jul 10. Acta Pharmacol Sin. 2018. PMID: 29991713 Free PMC article.
Evidence for a role for the p110-alpha isoform of PI3K in skeletal function.
Grey A, Chaussade C, Empson V, Lin JM, Watson M, O'Sullivan S, Rewcastle G, Naot D, Cornish J, Shepherd P. Grey A, et al. Biochem Biophys Res Commun. 2010 Jan 1;391(1):564-9. doi: 10.1016/j.bbrc.2009.11.099. Epub 2009 Nov 24. Biochem Biophys Res Commun. 2010. PMID: 19931507
Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors.
Rewcastle GW, Kolekar S, Buchanan CM, Gamage SA, Giddens AC, Tsang KY, Kendall JD, Singh R, Lee WJ, Smith GC, Han W, Matthews DJ, Denny WA, Shepherd PR, Jamieson SMF. Rewcastle GW, et al. Among authors: shepherd pr. Oncotarget. 2017 Jul 18;8(29):47725-47740. doi: 10.18632/oncotarget.17730. Oncotarget. 2017. PMID: 28537878 Free PMC article.
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