Free–Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of N‑Methylation for PI3Kδ Activity

Phosphoinositide-3-kinase δ (PI3Kδ) is a critical regulator of cell growth and transformation and has been explored as a therapeutic target for a range of diseases. Through the exploration of the thienopyrimidine scaffold, we have identified a ligand-efficient methylation that leads to remarkable se...

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Bibliographic Details

Published in:	Journal of medicinal chemistry Vol. 62; no. 22; pp. 10402 - 10422
Main Authors:	Barnes, Lydia, Blaber, Hollie, Brooks, David T. K, Byers, Lewis, Buckley, Daniel, Byron, Zoe C, Chilvers, Richard G, Cochrane, Liam, Cooney, Edward, Damian, Heather A, Francis, Luke, Fu He, Daniel, Grace, Jack M. J, Green, Harley J, Hogarth, Edmund J. P, Jusu, Leyla, Killalea, C. Elizabeth, King, Oliver, Lambert, Joseph, Lee, Zoe J, Lima, Nuria S, Long, Christina L, Mackinnon, May-Li, Mahdy, Shusha, Matthews-Wright, Jolyon, Millward, Makenzie J, Meehan, Matthew F, Merrett, Christopher, Morrison, Lisa, Parke, Hal R. I, Payne, Charlotte, Payne, Lawrence, Pike, Craig, Seal, Alexander, Senior, Aaron J, Smith, Keenan M, Stanelyte, Kamile, Stillibrand, Joe, Szpara, Rachel, Taday, Freya F. H, Threadgould, Antony M, Trainor, Rohan J, Waters, Jordan, Williams, Oliver, Wong, Carrie K. W, Wood, Katherine, Barton, Nick, Gruszka, Anna, Henley, Zoe, Rowedder, James E, Cookson, Rosa, Jones, Katherine L, Nadin, Alan, Smith, Ian E, Macdonald, Simon J. F, Nortcliffe, Andrew
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 27-11-2019
Online Access:	Get full text
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