BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib

Irreversible inhibitors of Bruton tyrosine kinase (BTK), pioneered by ibrutinib, have become breakthrough drugs in the treatment of leukemias and lymphomas. Resistance variants (mutations) occur, but in contrast to those identified for many other tyrosine kinase inhibitors, they affect less frequent...

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Publicado no:Leukemia
Main Authors: Estupiñán, H. Yesid, Wang, Qing, Berglöf, Anna, Schaafsma, Gerard C. P., Shi, Yuye, Zhou, Litao, Mohammad, Dara K., Yu, Liang, Vihinen, Mauno, Zain, Rula, Smith, C. I. Edvard
Formato: Artigo
Idioma:Inglês
Publicado em: Nature Publishing Group UK 2021
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8102192/
https://ncbi.nlm.nih.gov/pubmed/33526860
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41375-021-01123-6
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