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Rapid assessment of DCLK1 inhibitors using a peptide substrate mobility shift assay

Peptide mobility shift assays provide a sensitive measure of kinase enzymatic activity and can be used to evaluate kinase inhibitors. Herein, we describe a protocol adapted for rapid assessment of doublecortin-like kinase inhibitors. Advantages include rapid iterations of therapeutic compound assess...

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Detalles Bibliográficos
Autores principales: Liu, Yan, Westover, Kenneth D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8203847/
https://www.ncbi.nlm.nih.gov/pubmed/34159321
http://dx.doi.org/10.1016/j.xpro.2021.100587
Descripción
Sumario:Peptide mobility shift assays provide a sensitive measure of kinase enzymatic activity and can be used to evaluate kinase inhibitors. Herein, we describe a protocol adapted for rapid assessment of doublecortin-like kinase inhibitors. Advantages include rapid iterations of therapeutic compound assessment and the ability to characterize kinase mutations, such as drug-resistant mutants for biological rescue experiments, on kinase activity. For complete details on the use and execution of this protocol, please refer to Liu et al. (2020).