Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation.

Johnson, Eric; McTigue, Michele; Gallego, Rebecca A; Johnson, Ted W; Timofeevski, Sergei; Maestre, Michael; Fisher, Timothy S; Kania, Robert; Sawasdikosol, Sansana; Burakoff, Steven; Cronin, Ciarán N

Johnson, Eric; McTigue, Michele; Gallego, Rebecca A; Johnson, Ted W; Timofeevski, Sergei; Maestre, Michael; Fisher, Timothy S; Kania, Robert; Sawasdikosol, Sansana; Burakoff, Steven; Cronin, Ciarán N.

Afiliación

Johnson E; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
McTigue M; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
Gallego RA; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
Johnson TW; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
Timofeevski S; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
Maestre M; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
Fisher TS; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
Kania R; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and.
Sawasdikosol S; Department of Oncological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York 10029.
Burakoff S; Department of Oncological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York 10029.
Cronin CN; From the La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121 and ciaran.cronin@pfizer.com.

J Biol Chem ; 294(23): 9029-9036, 2019 06 07.

Article en En | MEDLINE | ID: mdl-31018963

Asunto(s)

Proteínas Serina-Treonina Quinasas/metabolismo; Sunitinib/metabolismo; Adenosina Trifosfato/química; Adenosina Trifosfato/metabolismo; Sitios de Unión; Cristalografía por Rayos X; Dimerización; Humanos; Interleucina-2/metabolismo; Simulación de Dinámica Molecular; Mutagénesis Sitio-Dirigida; Fosforilación; Proteínas Serina-Treonina Quinasas/antagonistas & inhibidores; Proteínas Serina-Treonina Quinasas/genética; Estructura Terciaria de Proteína; Proteínas Recombinantes/biosíntesis; Proteínas Recombinantes/química; Proteínas Recombinantes/genética; Sunitinib/química; Sunitinib/farmacología; Linfocitos T/citología; Linfocitos T/efectos de los fármacos; Linfocitos T/metabolismo

Palabras clave

cancer; conformational change; conformational plasticity; crystal structure; dimerization; domain swapping; drug discovery; hematopoietic progenitor kinase 1 (HPK1); inhibitor; serine/threonine protein kinase; trans-regulation

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Serina-Treonina Quinasas / Sunitinib Límite: Humans Idioma: En Revista: J Biol Chem Año: 2019 Tipo del documento: Article

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