BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to...
BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib
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London: Nature Publishing Group UK
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Language
English
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London: Nature Publishing Group UK
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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 frequently the “gatekeeper” residue in the catalytic domai...
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Full title
BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib
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TN_cdi_swepub_primary_oai_swepub_ki_se_464677
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https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_swepub_primary_oai_swepub_ki_se_464677
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ISSN
0887-6924
E-ISSN
1476-5551
DOI
10.1038/s41375-021-01123-6