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Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
La unión específica y saturable de pp60v-src a las membranas plasmáticas: evidencia de un receptor de miristilo-src
1Department of Biology, Princeton University, New Jersey 08544.
Cell
|July 28, 1989
Resumen
La proteína transformadora pp60v-src se une a las membranas plasmáticas a través del miristato en su extremo amino. Esta unión específica sugiere la presencia de un receptor dedicado en la superficie celular.
Área de la Ciencia:
- Biología Molecular Biología Molecular
- Biología celular Biología celular.
- Virología Virología.
Sus antecedentes:
- pp60v-src es la proteína transformadora del virus del sarcoma de Rous.
- Comprender su asociación de membrana es crucial para la oncogénesis viral.
Objetivo del estudio:
- Para investigar la base molecular de la asociación de la membrana pp60v-src.
- Identificar el mecanismo y la especificidad de la unión de pp60v-src a las membranas plasmáticas.
Principales métodos:
- La traducción in vitro del ARNm src para producir pp60v-src.
- Sistema libre de células que utiliza membranas plasmáticas y pp60v-src sintetizado.
- Ensayos de competencia con péptidos miristilados y no miristilados.
Principales resultados:
- El pp60v-src recién sintetizado se une rápidamente a las membranas plasmáticas.
- La unión fue saturable y dependiente de la miristoilación N-terminal.
- El tratamiento térmico o con tripsina de las membranas reduce la unión.
- El péptido src miristilado compitió en la unión, lo que indica especificidad.
Conclusiones:
- La miristoilación en el extremo N de pp60v-src es esencial para la asociación de la membrana.
- La evidencia sugiere la existencia de un receptor específico para pp60v-src en la membrana plasmática.
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