Selective Inhibition of Bruton’s Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors

[Image: see text] Bruton’s tyrosine kinase (BTK) is a member of the TEC-family kinases and crucial for the proliferation and differentiation of B-cells. We evaluated the therapeutic potential of a covalent inhibitor (JS25) with nanomolar potency against BTK and with a more desirable selectivity and...

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Autores principales: Sousa, Bárbara B., de Almeida, Cátia Rebelo, Barahona, Ana F., Lopes, Raquel, Martins-Logrado, Ana, Cavaco, Marco, Neves, Vera, Carvalho, Luís A. R., Labão-Almeida, Carlos, Coelho, Ana R., Leal Bento, Marta, Lopes, Ricardo M. R. M., Oliveira, Bruno L., Castanho, Miguel A. R. B., Neumeister, Peter, Deutsch, Alexander, Vladimer, Gregory I., Krall, Nikolaus, João, Cristina, Corzana, Francisco, Seixas, João D., Fior, Rita, Bernardes, Gonçalo J. L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9667546/
https://www.ncbi.nlm.nih.gov/pubmed/36407952
http://dx.doi.org/10.1021/acsptsci.2c00163

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