A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation.

Waizenegger, Irene C; Baum, Anke; Steurer, Steffen; Stadtmüller, Heinz; Bader, Gerd; Schaaf, Otmar; Garin-Chesa, Pilar; Schlattl, Andreas; Schweifer, Norbert; Haslinger, Christian; Colbatzky, Florian; Mousa, Sien; Kalkuhl, Arno; Kraut, Norbert; Adolf, Günther R

Waizenegger, Irene C; Baum, Anke; Steurer, Steffen; Stadtmüller, Heinz; Bader, Gerd; Schaaf, Otmar; Garin-Chesa, Pilar; Schlattl, Andreas; Schweifer, Norbert; Haslinger, Christian; Colbatzky, Florian; Mousa, Sien; Kalkuhl, Arno; Kraut, Norbert; Adolf, Günther R.

Afiliação

Waizenegger IC; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria. irene.waizenegger@boehringer-ingelheim.com.
Baum A; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Steurer S; Department of Medicinal Chemistry, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Stadtmüller H; Department of Medicinal Chemistry, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Bader G; Department of Medicinal Chemistry, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Schaaf O; Department of Discovery ADME, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Garin-Chesa P; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Schlattl A; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Schweifer N; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Haslinger C; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Colbatzky F; Department of Non-clinical Drug Safety, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach an der Riss, Germany.
Mousa S; Department of Non-clinical Drug Safety, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach an der Riss, Germany.
Kalkuhl A; Department of Non-clinical Drug Safety, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach an der Riss, Germany.
Kraut N; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Adolf GR; Department of Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.

Mol Cancer Ther ; 15(3): 354-65, 2016 Mar.

Article em En | MEDLINE | ID: mdl-26916115

Assuntos

Antineoplásicos/farmacologia; Mutação; Neoplasias/genética; Inibidores de Proteínas Quinases/farmacologia; Proteínas Proto-Oncogênicas B-raf/antagonistas & inibidores; Proteínas Proto-Oncogênicas B-raf/genética; Animais; Antineoplásicos/química; Biomarcadores; Linhagem Celular Tumoral; Proliferação de Células/efeitos dos fármacos; Modelos Animais de Doenças; Resistencia a Medicamentos Antineoplásicos; Ativação Enzimática/efeitos dos fármacos; Feminino; Humanos; Isoenzimas; Masculino; Camundongos; Modelos Moleculares; Conformação Molecular; Estrutura Molecular; Neoplasias/tratamento farmacológico; Neoplasias/metabolismo; Neoplasias/patologia; Inibidores de Proteínas Quinases/química; Multimerização Proteica; Proteínas Proto-Oncogênicas B-raf/química; Ratos; Ensaios Antitumorais Modelo de Xenoenxerto

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteínas Proto-Oncogênicas B-raf / Inibidores de Proteínas Quinases / Mutação / Neoplasias / Antineoplásicos Limite: Animals / Female / Humans / Male Idioma: En Ano de publicação: 2016 Tipo de documento: Article

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