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

Estupinan, HY; Wang, Q; Berglof, A; Schaafsma, GCP; Shi, YY; Zhou, LT; Mohammad, DK; Yu, L; Vihinen, M; Zain, R; Smith, CIE

Smith, CIE (corresponding author), Karolinska Univ Hosp Huddinge, Karolinska Inst, Clin Res Ctr, Dept Lab Med, SE-14186 Huddinge, Sweden.

LEUKEMIA, ; ():

Abstract

Irreversible inhibitors of Bruton tyrosine kinase (BTK), pioneered by ibrutinib, have become breakthrough drugs in the treatment of leukemias and lymp......

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