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Gatekeeper mutations activate FGF receptor tyrosine kinases by destabilizing the autoinhibited state

Many types of human cancers are being treated with small molecule ATP-competitive inhibitors targeting the kinase domain of receptor tyrosine kinases. Despite initial successful remission, long-term treatment almost inevitably leads to the emergence of drug resistance mutations at the gatekeeper res...

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Detalles Bibliográficos
Autores principales: Besch, Alida, Marsiglia, William M., Mohammadi, Moosa, Zhang, Yingkai, Traaseth, Nathaniel J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Academy of Sciences 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9974468/
https://www.ncbi.nlm.nih.gov/pubmed/36791110
http://dx.doi.org/10.1073/pnas.2213090120