ERK1/2 inhibitors act as monovalent degraders inducing ubiquitylation and proteasome-dependent turnover of ERK2, but not ERK1

Innate or acquired resistance to small molecule BRAF or MEK1/2 inhibitors (BRAFi or MEKi) typically arises through mechanisms that sustain or reinstate ERK1/2 activation. This has led to the development of a range of ERK1/2 inhibitors (ERKi) that either inhibit kinase catalytic activity (catERKi) or...

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Detalles Bibliográficos
Autores principales: Balmanno, Kathryn, Kidger, Andrew M., Byrne, Dominic P., Sale, Matthew J., Nassman, Nejma, Eyers, Patrick A., Cook, Simon J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Portland Press Ltd. 2023
Materias:
Cancer
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10212521/
https://www.ncbi.nlm.nih.gov/pubmed/37018014
http://dx.doi.org/10.1042/BCJ20220598

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