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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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Detalhes bibliográficos
Publicado no:J Biol Chem
Main Authors: Lippert, Lisa G., Ma, Ning, Ritt, Michael, Jain, Abhinandan, Vaidehi, Nagarajan, Sivaramakrishnan, Sivaraj
Formato: Artigo
Idioma:Inglês
Publicado em: American Society for Biochemistry and Molecular Biology 2021
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7949123/
https://ncbi.nlm.nih.gov/pubmed/33508318
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.jbc.2021.100339
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