Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.

Fairhurst, Robin A; Knoepfel, Thomas; Buschmann, Nicole; Leblanc, Catherine; Mah, Robert; Todorov, Milen; Nimsgern, Pierre; Ripoche, Sebastien; Niklaus, Michel; Warin, Nicolas; Luu, Van Huy; Madoerin, Mario; Wirth, Jasmin; Graus-Porta, Diana; Weiss, Andreas; Kiffe, Michael; Wartmann, Markus; Kinyamu-Akunda, Jacqueline; Sterker, Dario; Stamm, Christelle; Adler, Flavia; Buhles, Alexandra; Schadt, Heiko; Couttet, Philippe; Blank, Jutta; Galuba, Inga; Trappe, Jörg; Voshol, Johannes; Ostermann, Nils; Zou, Chao; Berghausen, Jörg; Del Rio Espinola, Alberto; Jahnke, Wolfgang; Furet, Pascal

Fairhurst, Robin A; Knoepfel, Thomas; Buschmann, Nicole; Leblanc, Catherine; Mah, Robert; Todorov, Milen; Nimsgern, Pierre; Ripoche, Sebastien; Niklaus, Michel; Warin, Nicolas; Luu, Van Huy; Madoerin, Mario; Wirth, Jasmin; Graus-Porta, Diana; Weiss, Andreas; Kiffe, Michael; Wartmann, Markus; Kinyamu-Akunda, Jacqueline; Sterker, Dario; Stamm, Christelle; Adler, Flavia; Buhles, Alexandra; Schadt, Heiko; Couttet, Philippe; Blank, Jutta; Galuba, Inga; Trappe, Jörg; Voshol, Johannes; Ostermann, Nils; Zou, Chao; Berghausen, Jörg; Del Rio Espinola, Alberto; Jahnke, Wolfgang; Furet, Pascal.

Afiliação

Fairhurst RA; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Knoepfel T; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Buschmann N; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Leblanc C; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Mah R; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Todorov M; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Nimsgern P; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Ripoche S; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Niklaus M; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Warin N; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Luu VH; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Madoerin M; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Wirth J; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Graus-Porta D; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Weiss A; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Kiffe M; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Wartmann M; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Kinyamu-Akunda J; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Sterker D; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Stamm C; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Adler F; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Buhles A; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Schadt H; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Couttet P; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Blank J; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Galuba I; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Trappe J; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Voshol J; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Ostermann N; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Zou C; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Berghausen J; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Del Rio Espinola A; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Jahnke W; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Furet P; Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.

J Med Chem ; 63(21): 12542-12573, 2020 11 12.

Article em En | MEDLINE | ID: mdl-32930584

Assuntos

Piperazinas/química; Inibidores de Proteínas Quinases/química; Piridinas/química; Receptor Tipo 4 de Fator de Crescimento de Fibroblastos/antagonistas & inibidores; Sequência de Aminoácidos; Animais; Sítios de Ligação; Linhagem Celular Tumoral; Proliferação de Células/efeitos dos fármacos; Cisteína/química; Cães; Desenho de Fármacos; Meia-Vida; Hepatócitos/citologia; Hepatócitos/efeitos dos fármacos; Hepatócitos/metabolismo; Neoplasias Hepáticas/tratamento farmacológico; Camundongos; Microssomos Hepáticos/metabolismo; Simulação de Dinâmica Molecular; Piperazinas/metabolismo; Piperazinas/farmacologia; Piperazinas/uso terapêutico; Inibidores de Proteínas Quinases/metabolismo; Inibidores de Proteínas Quinases/farmacologia; Inibidores de Proteínas Quinases/uso terapêutico; Piridinas/metabolismo; Piridinas/farmacologia; Piridinas/uso terapêutico; Ratos; Receptor Tipo 4 de Fator de Crescimento de Fibroblastos/metabolismo; Relação Estrutura-Atividade; Ensaios Antitumorais Modelo de Xenoenxerto

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Piridinas / Inibidores de Proteínas Quinases / Receptor Tipo 4 de Fator de Crescimento de Fibroblastos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Suíça

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