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Kinase inhibitors allosterically disrupt a regulatory interaction to enhance PKCα membrane translocation

The eukaryotic kinase domain has multiple intrinsically disordered regions whose conformation dictates kinase activity. Small molecule kinase inhibitors (SMKIs) rely on disrupting the active conformations of these disordered regions to inactivate the kinase. While SMKIs are selected for their abilit...

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Detalles Bibliográficos
Autores principales:	Lippert, Lisa G., Ma, Ning, Ritt, Michael, Jain, Abhinandan, Vaidehi, Nagarajan, Sivaramakrishnan, Sivaraj
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Society for Biochemistry and Molecular Biology 2021
Materias:	Research Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7949123/ https://www.ncbi.nlm.nih.gov/pubmed/33508318 http://dx.doi.org/10.1016/j.jbc.2021.100339

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