| Autor: |
Lydia, Barnes, Hollie, Blaber, David T K, Brooks, Lewis, Byers, Daniel, Buckley, Zoe C, Byron, Richard G, Chilvers, Liam, Cochrane, Edward, Cooney, Heather A, Damian, Luke, Francis, Daniel, Fu He, Jack M J, Grace, Harley J, Green, Edmund J P, Hogarth, Leyla, Jusu, C Elizabeth, Killalea, Oliver, King, Joseph, Lambert, Zoe J, Lee, Nuria S, Lima, Christina L, Long, May-Li, Mackinnon, Shusha, Mahdy, Jolyon, Matthews-Wright, Makenzie J, Millward, Matthew F, Meehan, Christopher, Merrett, Lisa, Morrison, Hal R I, Parke, Charlotte, Payne, Lawrence, Payne, Craig, Pike, Alexander, Seal, Aaron J, Senior, Keenan M, Smith, Kamile, Stanelyte, Joe, Stillibrand, Rachel, Szpara, Freya F H, Taday, Antony M, Threadgould, Rohan J, Trainor, Jordan, Waters, Oliver, Williams, Carrie K W, Wong, Katherine, Wood, Nick, Barton, Anna, Gruszka, Zoe, Henley, James E, Rowedder, Rosa, Cookson, Katherine L, Jones, Alan, Nadin, Ian E, Smith, Simon J F, Macdonald, Andrew, Nortcliffe |
| Rok vydání: |
2019 |
| Předmět: |
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| Zdroj: |
Journal of medicinal chemistry. 62(22) |
| ISSN: |
1520-4804 |
| Popis: |
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 selectivity for PI3Kδ over the closely related isoforms. Interrogation through the Free-Wilson analysis highlights the innate selectivity the thienopyrimidine scaffold has for PI3Kδ and provides a predictive model for the activity against the PI3K isoforms. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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