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Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ.
Collier, Philip N; Messersmith, David; Le Tiran, Arnaud; Bandarage, Upul K; Boucher, Christina; Come, Jon; Cottrell, Kevin M; Damagnez, Veronique; Doran, John D; Griffith, James P; Khare-Pandit, Suvarna; Krueger, Elaine B; Ledeboer, Mark W; Ledford, Brian; Liao, Yusheng; Mahajan, Sudipta; Moody, Cameron S; Roday, Setu; Wang, Tiansheng; Xu, Jinwang; Aronov, Alex M.
Afiliação
  • Collier PN; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Messersmith D; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Le Tiran A; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Bandarage UK; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Boucher C; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Come J; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Cottrell KM; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Damagnez V; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Doran JD; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Griffith JP; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Khare-Pandit S; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Krueger EB; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Ledeboer MW; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Ledford B; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Liao Y; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Mahajan S; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Moody CS; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Roday S; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Wang T; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Xu J; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
  • Aronov AM; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.
J Med Chem ; 58(14): 5684-8, 2015 Jul 23.
Article em En | MEDLINE | ID: mdl-26121481
ABSTRACT
A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase structure. Optimization of the alkylimidazole group led to inhibitors with higher levels of PI3Kγ selectivity. Additional insights into PI3K isoform selectivity related to sequence differences in a known distal hydrophobic pocket are also described.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperidinas / Inibidores Enzimáticos / Descoberta de Drogas / Inibidores de Fosfoinositídeo-3 Quinase Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
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PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperidinas / Inibidores Enzimáticos / Descoberta de Drogas / Inibidores de Fosfoinositídeo-3 Quinase Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Estados Unidos