Chemical Editing of Macrocyclic Natural Products and Kinetic Profiling Reveal Slow, Tight-Binding Histone Deacetylase Inhibitors with Picomolar Affinities.

Kitir, Betül; Maolanon, Alex R; Ohm, Ragnhild G; Colaço, Ana R; Fristrup, Peter; Madsen, Andreas S; Olsen, Christian A

Kitir, Betül; Maolanon, Alex R; Ohm, Ragnhild G; Colaço, Ana R; Fristrup, Peter; Madsen, Andreas S; Olsen, Christian A.

Afiliação

Kitir B; Center for Biopharmaceuticals and Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Maolanon AR; Center for Biopharmaceuticals and Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Ohm RG; Center for Biopharmaceuticals and Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Colaço AR; Department of Chemistry, Technical University of Denmark , DK-2800 Kongens Lyngby, Denmark.
Fristrup P; Department of Chemistry, Technical University of Denmark , DK-2800 Kongens Lyngby, Denmark.
Madsen AS; Center for Biopharmaceuticals and Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.
Olsen CA; Center for Biopharmaceuticals and Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen , DK-2100 Copenhagen, Denmark.

Biochemistry ; 56(38): 5134-5146, 2017 09 26.

Article em En | MEDLINE | ID: mdl-28858522

Assuntos

Produtos Biológicos/química; Inibidores de Histona Desacetilases/química; Inibidores de Histona Desacetilases/farmacologia; Compostos Macrocíclicos/química; Antineoplásicos/síntese química; Antineoplásicos/química; Antineoplásicos/farmacologia; Técnicas de Química Sintética; Relação Dose-Resposta a Droga; Células HeLa; Inibidores de Histona Desacetilases/administração & dosagem; Histona Desacetilases/metabolismo; Humanos; Cinética; Compostos Macrocíclicos/síntese química; Compostos Macrocíclicos/farmacologia; Pró-Fármacos/farmacologia; Proteínas Recombinantes/genética; Proteínas Recombinantes/metabolismo; Relação Estrutura-Atividade; Zinco/metabolismo

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Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Produtos Biológicos / Compostos Macrocíclicos / Inibidores de Histona Desacetilases Limite: Humans Idioma: En Revista: Biochemistry Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Dinamarca

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