Discovery and characterization of an iminocoumarin scaffold as an inhibitor of MEKK2 (MAP3K2).

Ahmad, Syed; St Hilaire, Valentine R; Dandepally, Srinivasa R; Johnson, Gary L; Williams, Alfred L; Scott, John E

Ahmad, Syed; St Hilaire, Valentine R; Dandepally, Srinivasa R; Johnson, Gary L; Williams, Alfred L; Scott, John E.

Afiliação

Ahmad S; Department of Pharmaceutical Sciences, Biomanufacturing Research Institute and Technology Enterprise (BRITE), North Carolina Central University, Durham, NC, USA.
St Hilaire VR; Department of Pharmaceutical Sciences, Biomanufacturing Research Institute and Technology Enterprise (BRITE), North Carolina Central University, Durham, NC, USA.
Dandepally SR; Department of Pharmaceutical Sciences, Biomanufacturing Research Institute and Technology Enterprise (BRITE), North Carolina Central University, Durham, NC, USA.
Johnson GL; Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC, USA; Lineberger Comprehensive Cancer Center, University of North Carolina School of Medicine, Chapel Hill, NC, USA.
Williams AL; Department of Pharmaceutical Sciences, Biomanufacturing Research Institute and Technology Enterprise (BRITE), North Carolina Central University, Durham, NC, USA.
Scott JE; Department of Pharmaceutical Sciences, Biomanufacturing Research Institute and Technology Enterprise (BRITE), North Carolina Central University, Durham, NC, USA. Electronic address: jscott@nccu.edu.

Biochem Biophys Res Commun ; 496(1): 205-211, 2018 01 29.

Article em En | MEDLINE | ID: mdl-29309787

Assuntos

Cumarínicos/química; Cumarínicos/metabolismo; MAP Quinase Quinase Quinase 2/antagonistas & inibidores; MAP Quinase Quinase Quinase 2/metabolismo; Mapeamento de Interação de Proteínas/métodos; Inibidores de Proteínas Quinases/química; Inibidores de Proteínas Quinases/metabolismo; Células Cultivadas; Cumarínicos/administração & dosagem; Sistemas de Liberação de Medicamentos/métodos; Descoberta de Drogas; Avaliação Pré-Clínica de Medicamentos/métodos; Humanos; Inibidores de Proteínas Quinases/administração & dosagem

Palavras-chave

ADP; ATP; DMSO; ELISA; HTS; Inhibitor; Kinase; MAP3K2; MAPK; MEKK2; MS; SAR; SD; TR-FRET; adenosine diphosphate; adenosine triphosphate; dimethyl sulfoxide; enzyme-linked immunosorbent assay; high throughput screening; mass spectrometry; mitogen-activated protein kinase; standard deviation; structure-activity relationship; time-resolved fluorescence resonance energy transfer

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Cumarínicos / Mapeamento de Interação de Proteínas / MAP Quinase Quinase Quinase 2 / Inibidores de Proteínas Quinases Limite: Humans Idioma: En Revista: Biochem Biophys Res Commun Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Estados Unidos

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