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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Bibliographic Details
Published in: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
Format: Artigo
Language:Inglês
Published: Nature Publishing Group UK 2021
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Online Access: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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