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Discovery of 4-Azaindole Inhibitors of TGFßRI as Immuno-oncology Agents.
Zhang, Yong; Zhao, Yufen; Tebben, Andrew J; Sheriff, Steven; Ruzanov, Max; Fereshteh, Mark P; Fan, Yi; Lippy, Jonathan; Swanson, Jesse; Ho, Ching-Ping; Wautlet, Barri S; Rose, Anne; Parrish, Karen; Yang, Zheng; Donnell, Andrew F; Zhang, Liping; Fink, Brian E; Vite, Gregory D; Augustine-Rauch, Karen; Fargnoli, Joseph; Borzilleri, Robert M.
Afiliação
  • Zhang Y; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Zhao Y; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Tebben AJ; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Sheriff S; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Ruzanov M; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Fereshteh MP; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Fan Y; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Lippy J; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Swanson J; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Ho CP; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Wautlet BS; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Rose A; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Parrish K; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Yang Z; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Donnell AF; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Zhang L; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Fink BE; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Vite GD; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Augustine-Rauch K; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Fargnoli J; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
  • Borzilleri RM; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, New Jersey 08543, United States.
ACS Med Chem Lett ; 9(11): 1117-1122, 2018 Nov 08.
Article em En | MEDLINE | ID: mdl-30429955
ABSTRACT
The multifunctional cytokine TGFß plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFß signaling in concert with checkpoint blockade will provide improved and durable immune response against tumors. Herein, we describe a novel series of 4-azaindole TGFß receptor kinase inhibitors with excellent selectivity for TGFß receptor 1 kinase. The combination of compound 3f and an antimouse-PD-1 antibody demonstrated significantly improved antitumor efficacy compared to either treatment alone in a murine tumor model.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Estados Unidos