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Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
Albrecht, Brian K; Gehling, Victor S; Hewitt, Michael C; Vaswani, Rishi G; Côté, Alexandre; Leblanc, Yves; Nasveschuk, Christopher G; Bellon, Steve; Bergeron, Louise; Campbell, Robert; Cantone, Nico; Cooper, Michael R; Cummings, Richard T; Jayaram, Hariharan; Joshi, Shivangi; Mertz, Jennifer A; Neiss, Adrianne; Normant, Emmanuel; O'Meara, Michael; Pardo, Eneida; Poy, Florence; Sandy, Peter; Supko, Jeffrey; Sims, Robert J; Harmange, Jean-Christophe; Taylor, Alexander M; Audia, James E.
Afiliação
  • Albrecht BK; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Gehling VS; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Hewitt MC; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Vaswani RG; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Côté A; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Leblanc Y; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Nasveschuk CG; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Bellon S; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Bergeron L; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Campbell R; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cantone N; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cooper MR; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cummings RT; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Jayaram H; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Joshi S; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Mertz JA; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Neiss A; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Normant E; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • O'Meara M; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Pardo E; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Poy F; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Sandy P; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Supko J; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Sims RJ; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Harmange JC; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Taylor AM; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Audia JE; Constellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
J Med Chem ; 59(4): 1330-9, 2016 Feb 25.
Article em En | MEDLINE | ID: mdl-26815195
ABSTRACT
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising approach to regulate the expression of important disease-relevant genes, including MYC, BCL-2, and NF-κB. Here we describe the identification and characterization of a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor that attenuates BET-dependent gene expression in vivo, demonstrates antitumor efficacy in an MV-4-11 mouse xenograft model, and is currently undergoing human clinical trials for hematological malignancies (CPI-0610).
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Azepinas / Fatores de Transcrição / Proteínas Nucleares / Leucemia Mieloide Aguda / Regulação Neoplásica da Expressão Gênica / Antineoplásicos Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals / Humans Idioma: En Revista: J Med Chem Ano de publicação: 2016 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Azepinas / Fatores de Transcrição / Proteínas Nucleares / Leucemia Mieloide Aguda / Regulação Neoplásica da Expressão Gênica / Antineoplásicos Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals / Humans Idioma: En Revista: J Med Chem Ano de publicação: 2016 Tipo de documento: Article