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Differential impact of BTK active site inhibitors on the conformational state of full-length BTK

Bruton’s tyrosine kinase (BTK) is targeted in the treatment of B-cell disorders including leukemias and lymphomas. Currently approved BTK inhibitors, including Ibrutinib, a first-in-class covalent inhibitor of BTK, bind directly to the kinase active site. While effective at blocking the catalytic ac...

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Detalles Bibliográficos
Autores principales: Joseph, Raji E, Amatya, Neha, Fulton, D Bruce, Engen, John R, Wales, Thomas E, Andreotti, Amy
Formato: Online Artículo Texto
Lenguaje:English
Publicado: eLife Sciences Publications, Ltd 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7834017/
https://www.ncbi.nlm.nih.gov/pubmed/33226337
http://dx.doi.org/10.7554/eLife.60470