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ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia.
Maes, Tamara; Mascaró, Cristina; Tirapu, Iñigo; Estiarte, Angels; Ciceri, Filippo; Lunardi, Serena; Guibourt, Nathalie; Perdones, Alvaro; Lufino, Michele M P; Somervaille, Tim C P; Wiseman, Dan H; Duy, Cihangir; Melnick, Ari; Willekens, Christophe; Ortega, Alberto; Martinell, Marc; Valls, Nuria; Kurz, Guido; Fyfe, Matthew; Castro-Palomino, Julio Cesar; Buesa, Carlos.
Afiliação
  • Maes T; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain. Electronic address: tmaes@oryzon.com.
  • Mascaró C; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Tirapu I; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Estiarte A; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Ciceri F; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Lunardi S; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Guibourt N; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Perdones A; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Lufino MMP; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Somervaille TCP; Leukaemia Biology Laboratory, Cancer Research UK Manchester Institute, The University of Manchester, Manchester M20 4BX, UK.
  • Wiseman DH; Leukaemia Biology Laboratory, Cancer Research UK Manchester Institute, The University of Manchester, Manchester M20 4BX, UK.
  • Duy C; Department of Medicine, Division of Hematology & Medical Oncology, Weill Cornell Medicine, New York, 10065 NY, USA.
  • Melnick A; Department of Medicine, Division of Hematology & Medical Oncology, Weill Cornell Medicine, New York, 10065 NY, USA; Department of Pharmacology, Weill Cornell Medicine, New York, 10065 NY, USA.
  • Willekens C; Drug Development Department (DITEP) and Hematology Department, Gustave Roussy, Université Paris-Saclay, 94805 Villejuif, France.
  • Ortega A; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Martinell M; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Valls N; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Kurz G; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Fyfe M; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Castro-Palomino JC; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
  • Buesa C; Oryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornellà de Llobregat, Spain.
Cancer Cell ; 33(3): 495-511.e12, 2018 03 12.
Article em En | MEDLINE | ID: mdl-29502954
ABSTRACT
The lysine-specific demethylase KDM1A is a key regulator of stem cell potential in acute myeloid leukemia (AML). ORY-1001 is a highly potent and selective KDM1A inhibitor that induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML. ORY-1001 exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of an AML xenograft model, and extends survival in a mouse PDX (patient-derived xenograft) model of T cell acute leukemia. Surrogate pharmacodynamic biomarkers developed based on expression changes in leukemia cell lines were translated to samples from patients treated with ORY-1001. ORY-1001 is a selective KDM1A inhibitor in clinical trials and is currently being evaluated in patients with leukemia and solid tumors.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Leucemia Mieloide Aguda / Diferenciação Celular / Histona Desmetilases Limite: Animals / Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Leucemia Mieloide Aguda / Diferenciação Celular / Histona Desmetilases Limite: Animals / Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article