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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...

https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_swepub_primary_oai_swepub_ki_se_464677

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

About this item

Full title

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

Publisher

London: Nature Publishing Group UK

Journal title

Leukemia, 2021-05, Vol.35 (5), p.1317-1329

Language

English

Formats

Publication information

Publisher

London: Nature Publishing Group UK

More information

Scope and Contents

Contents

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...

Alternative Titles

Full title

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

Identifiers

Primary Identifiers

Record Identifier

TN_cdi_swepub_primary_oai_swepub_ki_se_464677

Permalink

https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_swepub_primary_oai_swepub_ki_se_464677

Other Identifiers

ISSN

0887-6924

E-ISSN

1476-5551

DOI

10.1038/s41375-021-01123-6