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An Internally Controlled Quantitative Target Occupancy Assay for Covalent Inhibitors

Assessing target occupancy is critical for establishing proof-of-mechanism for novel inhibitors and to determine whether robust target inhibition can be achieved at tolerated doses. This is challenging in the clinic using conventional methods due to the need for untreated controls. We describe a new...

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Detalles Bibliográficos
Autores principales: Hansen, Rasmus, Firdaus, Sarah J., Li, Shuangwei, Janes, Matthew R., Zhang, Jingchuan, Liu, Yi, Zarrinkar, Patrick P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6156402/
https://www.ncbi.nlm.nih.gov/pubmed/30254226
http://dx.doi.org/10.1038/s41598-018-32683-w