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Discovery of highly potent, selective, covalent inhibitors of JAK3.
Kempson, James; Ovalle, Damaso; Guo, Junqing; Wrobleski, Stephen T; Lin, Shuqun; Spergel, Steven H; Duan, James J-W; Jiang, Bin; Lu, Zhonghui; Das, Jagabandhu; Yang, Bingwei V; Hynes, John; Wu, Hong; Tokarski, John; Sack, John S; Khan, Javed; Schieven, Gary; Blatt, Yuval; Chaudhry, Charu; Salter-Cid, Luisa M; Fura, Aberra; Barrish, Joel C; Carter, Percy H; Pitts, William J.
Afiliación
  • Kempson J; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA. Electronic address: james.kempson@bms.com.
  • Ovalle D; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Guo J; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Wrobleski ST; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Lin S; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Spergel SH; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Duan JJ; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Jiang B; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Lu Z; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Das J; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Yang BV; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Hynes J; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Wu H; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Tokarski J; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Sack JS; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Khan J; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Schieven G; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Blatt Y; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Chaudhry C; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Salter-Cid LM; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Fura A; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Barrish JC; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Carter PH; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
  • Pitts WJ; Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
Bioorg Med Chem Lett ; 27(20): 4622-4625, 2017 10 15.
Article en En | MEDLINE | ID: mdl-28927786
A useful and novel set of tool molecules have been identified which bind irreversibly to the JAK3 active site cysteine residue. The design was based on crystal structure information and a comparative study of several electrophilic warheads.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Inhibidores de Proteínas Quinasas / Janus Quinasa 3 Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article
Texto completo
Imprimir
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PubMed Links
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Inhibidores de Proteínas Quinasas / Janus Quinasa 3 Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article