Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors.

Niessen, Sherry; Dix, Melissa M; Barbas, Sabrina; Potter, Zachary E; Lu, Shuyan; Brodsky, Oleg; Planken, Simon; Behenna, Douglas; Almaden, Chau; Gajiwala, Ketan S; Ryan, Kevin; Ferre, RoseAnn; Lazear, Michael R; Hayward, Matthew M; Kath, John C; Cravatt, Benjamin F

Niessen, Sherry; Dix, Melissa M; Barbas, Sabrina; Potter, Zachary E; Lu, Shuyan; Brodsky, Oleg; Planken, Simon; Behenna, Douglas; Almaden, Chau; Gajiwala, Ketan S; Ryan, Kevin; Ferre, RoseAnn; Lazear, Michael R; Hayward, Matthew M; Kath, John C; Cravatt, Benjamin F.

Afiliação

Niessen S; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA; Oncology RU, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA. Electronic addre
Dix MM; Department of Molecular Medicine, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA.
Barbas S; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Potter ZE; Department of Molecular Medicine, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA.
Lu S; Drug Safety Research and Development, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Brodsky O; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Planken S; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Behenna D; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Almaden C; Oncology RU, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Gajiwala KS; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Ryan K; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Ferre R; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Lazear MR; Department of Molecular Medicine, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA.
Hayward MM; Discovery Sciences, Pfizer Worldwide Research and Development, MS 8220-2226 Eastern Point Road, Groton, CT 06340, USA.
Kath JC; Worldwide Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, USA.
Cravatt BF; Department of Molecular Medicine, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA. Electronic address: cravatt@scripps.edu.

Cell Chem Biol ; 24(11): 1388-1400.e7, 2017 Nov 16.

Article em En | MEDLINE | ID: mdl-28965727

Assuntos

Receptores ErbB/metabolismo; Inibidores de Proteínas Quinases/química; Proteoma/análise; 5'-Nucleotidase/química; 5'-Nucleotidase/genética; 5'-Nucleotidase/metabolismo; Acrilamidas; Compostos de Anilina; Animais; Catepsinas/química; Catepsinas/metabolismo; Linhagem Celular Tumoral; Quinase do Ponto de Checagem 2/química; Quinase do Ponto de Checagem 2/genética; Quinase do Ponto de Checagem 2/metabolismo; Cisteína/química; Receptores ErbB/genética; Proteínas Ligadas por GPI/química; Proteínas Ligadas por GPI/genética; Proteínas Ligadas por GPI/metabolismo; Células HEK293; Humanos; Fígado/metabolismo; Lisossomos/metabolismo; Camundongos; Camundongos Endogâmicos C57BL; Mutagênese Sítio-Dirigida; Piperazinas/química; Piperazinas/metabolismo; Inibidores de Proteínas Quinases/metabolismo; Proteômica; Rodaminas/química; Transplante Heterólogo

Palavras-chave

T790M-EGFR; cathepsins; chemical probes; covalent inhibitors; kinases; lysosomal accumulation; proteomics

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteoma / Inibidores de Proteínas Quinases / Receptores ErbB Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Revista: Cell Chem Biol Ano de publicação: 2017 Tipo de documento: Article

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