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ATP-competitive inhibitors of PI3K enzymes demonstrate an isoform selective dual action by controlling membrane binding.
Gong GQ, Masson GR, Lee WJ, Dickson JM, Kendall JD, Rathinaswamy MK, Buchanan CM, Middleditch M, Owen B, Spicer JA, Rewcastle GW, Denny WA, Burke JE, Shepherd PR, Williams RL, Flanagan JU. Gong GQ, et al. Among authors: rewcastle gw. Biochem J. 2024 Nov 1:BCJ20240479. doi: 10.1042/BCJ20240479. Online ahead of print. Biochem J. 2024. PMID: 39485310
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: rewcastle gw. 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
83 results