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Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of N-Methylation for PI3Kδ Activity.
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.
Afiliação
  • Barnes L; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Blaber H; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Brooks DTK; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Byers L; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Buckley D; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Byron ZC; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Chilvers RG; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Cochrane L; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Cooney E; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Damian HA; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Francis L; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Fu He D; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Grace JMJ; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Green HJ; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Hogarth EJP; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Jusu L; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Killalea CE; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • King O; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Lambert J; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Lee ZJ; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Lima NS; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Long CL; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Mackinnon ML; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Mahdy S; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Matthews-Wright J; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Millward MJ; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Meehan MF; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Merrett C; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Morrison L; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Parke HRI; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Payne C; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Payne L; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Pike C; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Seal A; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Senior AJ; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Smith KM; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Stanelyte K; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Stillibrand J; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Szpara R; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Taday FFH; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Threadgould AM; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Trainor RJ; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Waters J; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Williams O; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Wong CKW; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Wood K; GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
  • Barton N; GlaxoSmithKline, Medicines Research Centre , Gunnels Wood Road , Stevenage SG1 2NY , U.K.
  • Gruszka A; GlaxoSmithKline, Medicines Research Centre , Gunnels Wood Road , Stevenage SG1 2NY , U.K.
  • Henley Z; GlaxoSmithKline, Medicines Research Centre , Gunnels Wood Road , Stevenage SG1 2NY , U.K.
  • Rowedder JE; GlaxoSmithKline, Medicines Research Centre , Gunnels Wood Road , Stevenage SG1 2NY , U.K.
J Med Chem ; 62(22): 10402-10422, 2019 11 27.
Article em En | MEDLINE | ID: mdl-31647659
ABSTRACT
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Relação Estrutura-Atividade / Fosfatidilinositol 3-Quinases / Inibidores de Fosfoinositídeo-3 Quinase Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Reino Unido
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Relação Estrutura-Atividade / Fosfatidilinositol 3-Quinases / Inibidores de Fosfoinositídeo-3 Quinase Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Reino Unido