Chemoprobe-based assays of histone lysine demethylase 1A target occupation enable <i>in vivo</i> pharmacokinetics and pharmacodynamics studies of KDM1A inhibitors.

Mascaró, Cristina; Ortega, Alberto; Carceller, Elena; Ruiz Rodriguez, Raquel; Ciceri, Filippo; Lunardi, Serena; Yu, Li; Hilbert, Manuel; Maes, Tamara

Chemoprobe-based assays of histone lysine demethylase 1A target occupation enable in vivo pharmacokinetics and pharmacodynamics studies of KDM1A inhibitors.

Mascaró, Cristina; Ortega, Alberto; Carceller, Elena; Ruiz Rodriguez, Raquel; Ciceri, Filippo; Lunardi, Serena; Yu, Li; Hilbert, Manuel; Maes, Tamara.

Afiliação

Mascaró C; From Oryzon Genomics S.A., Carrer Sant Ferran 74, Cornellà de Llobregat, Barcelona 08940, Spain.
Ortega A; From Oryzon Genomics S.A., Carrer Sant Ferran 74, Cornellà de Llobregat, Barcelona 08940, Spain.
Carceller E; From Oryzon Genomics S.A., Carrer Sant Ferran 74, Cornellà de Llobregat, Barcelona 08940, Spain.
Ruiz Rodriguez R; From Oryzon Genomics S.A., Carrer Sant Ferran 74, Cornellà de Llobregat, Barcelona 08940, Spain.
Ciceri F; From Oryzon Genomics S.A., Carrer Sant Ferran 74, Cornellà de Llobregat, Barcelona 08940, Spain.
Lunardi S; From Oryzon Genomics S.A., Carrer Sant Ferran 74, Cornellà de Llobregat, Barcelona 08940, Spain.
Yu L; Roche Innovation Center New York, New York, New York 10016.
Hilbert M; Roche Innovation Center Basel, Grenzacherstrasse 124, Basel 4070, Switzerland.
Maes T; From Oryzon Genomics S.A., Carrer Sant Ferran 74, Cornellà de Llobregat, Barcelona 08940, Spain. Electronic address: tmaes@oryzon.com.

J Biol Chem ; 294(20): 8311-8322, 2019 05 17.

Article em En | MEDLINE | ID: mdl-30804215

Assuntos

Inibidores Enzimáticos; Histona Desmetilases/antagonistas & inibidores; Histona Desmetilases/metabolismo; Inibidores Enzimáticos/química; Inibidores Enzimáticos/farmacocinética; Inibidores Enzimáticos/farmacologia; Humanos; Células THP-1

Palavras-chave

FAD; chemoprobe; chemoproteomics; chromatin modification; drug development; enzyme inactivation; epigenetics; histone demethylase; histone lysine demethylase (KDM); lysine demethylase; pharmacokinetics; protein-drug interaction; target engagement; translational studies

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Histona Desmetilases Limite: Humans Idioma: En Revista: J Biol Chem Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Espanha

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