Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.

Kettle, Jason G; Ballard, Peter; Bardelle, Catherine; Cockerill, Mark; Colclough, Nicola; Critchlow, Susan E; Debreczeni, Judit; Fairley, Gary; Fillery, Shaun; Graham, Mark A; Goodwin, Louise; Guichard, Sylvie; Hudson, Kevin; Ward, Richard A; Whittaker, David

Kettle, Jason G; Ballard, Peter; Bardelle, Catherine; Cockerill, Mark; Colclough, Nicola; Critchlow, Susan E; Debreczeni, Judit; Fairley, Gary; Fillery, Shaun; Graham, Mark A; Goodwin, Louise; Guichard, Sylvie; Hudson, Kevin; Ward, Richard A; Whittaker, David.

Afiliação

Kettle JG; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Ballard P; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Bardelle C; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Cockerill M; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Colclough N; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Critchlow SE; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Debreczeni J; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Fairley G; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Fillery S; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Graham MA; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Goodwin L; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Guichard S; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Hudson K; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Ward RA; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Whittaker D; Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.

J Med Chem ; 58(6): 2834-44, 2015 Mar 26.

Article em En | MEDLINE | ID: mdl-25738750

ABSTRACT

ABSTRACT

Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response.

Assuntos

Inibidores de Proteínas Quinases/química; Inibidores de Proteínas Quinases/farmacologia; Proteínas Serina-Treonina Quinases/antagonistas & inibidores; Proteínas Tirosina Quinases/antagonistas & inibidores; Animais; Células COS; Linhagem Celular Tumoral; Chlorocebus aethiops; Descoberta de Drogas; Resistência a Medicamentos; Humanos; MAP Quinase Quinase Quinases/antagonistas & inibidores; MAP Quinase Quinase Quinases/metabolismo; Modelos Moleculares; Inibidores de Proteínas Quinases/farmacocinética; Proteínas Serina-Treonina Quinases/química; Proteínas Serina-Treonina Quinases/genética; Proteínas Serina-Treonina Quinases/metabolismo; Proteínas Tirosina Quinases/química; Proteínas Tirosina Quinases/genética; Proteínas Tirosina Quinases/metabolismo; Interferência de RNA; RNA Interferente Pequeno/genética; Ratos Wistar; Quinases Dyrk

Texto completo

Adicionar na Minha BVS

Imprimir

XML

PubMed Links

Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteínas Tirosina Quinases / Proteínas Serina-Treonina Quinases / Inibidores de Proteínas Quinases Limite: Animals / Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Reino Unido

Texto completo

Adicionar na Minha BVS

Imprimir

XML

PubMed Links

Buscar no Google