Microsecond simulations to investigate the structural mechanism of super-resistant double mutations in BTK to the covalent inhibitor ibrutinib in multiple leukemia.

Abstract excerpt

Bruton’s Tyrosine Kinase (BTK) is an anchor in B-cell receptor signaling and plays an important role in chronic lymphocytic leukemia (CLL). The use of covalent inhibitors of BTK, such as ibrutinib, enhances the survival of patients with CLL. However, mutations at the C481 residue cause resistance to ibrutinib and diminish its clinical efficacy. Recently, super-resistant mutants, i.e., T474M-C481S and T474I-C481S,...

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