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Page 1
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: lee wj. 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: lee wj. 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.
Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).
Rewcastle GW, Gamage SA, Flanagan JU, Frederick R, Denny WA, Baguley BC, Kestell P, Singh R, Kendall JD, Marshall ES, Lill CL, Lee WJ, Kolekar S, Buchanan CM, Jamieson SM, Shepherd PR. Rewcastle GW, et al. Among authors: lee wj. J Med Chem. 2011 Oct 27;54(20):7105-26. doi: 10.1021/jm200688y. Epub 2011 Sep 27. J Med Chem. 2011. PMID: 21882832
Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.
Kendall JD, O'Connor PD, Marshall AJ, Frédérick R, Marshall ES, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR. Kendall JD, et al. Among authors: lee wj. Bioorg Med Chem. 2012 Jan 1;20(1):69-85. doi: 10.1016/j.bmc.2011.11.029. Epub 2011 Nov 25. Bioorg Med Chem. 2012. PMID: 22177405
Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.
Kendall JD, Giddens AC, Tsang KY, Frédérick R, Marshall ES, Singh R, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR. Kendall JD, et al. Among authors: lee wj. Bioorg Med Chem. 2012 Jan 1;20(1):58-68. doi: 10.1016/j.bmc.2011.11.031. Epub 2011 Nov 25. Bioorg Med Chem. 2012. PMID: 22177407
Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
Marshall AJ, Lill CL, Chao M, Kolekar SV, Lee WJ, Marshall ES, Baguley BC, Shepherd PR, Denny WA, Flanagan JU, Rewcastle GW. Marshall AJ, et al. Among authors: lee wj. Bioorg Med Chem. 2015 Jul 1;23(13):3796-808. doi: 10.1016/j.bmc.2015.03.073. Epub 2015 Apr 4. Bioorg Med Chem. 2015. PMID: 25890698
Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110α-selective PI3 kinase inhibitors.
Kendall JD, Giddens AC, Tsang KY, Marshall ES, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Jamieson SMF, Rewcastle GW, Baguley BC, Denny WA, Shepherd PR. Kendall JD, et al. Among authors: lee wj. Bioorg Med Chem Lett. 2017 Jan 15;27(2):187-190. doi: 10.1016/j.bmcl.2016.11.078. Epub 2016 Nov 25. Bioorg Med Chem Lett. 2017. PMID: 27923617
4,359 results