Article
Novel mouse model resistant to irreversible BTK inhibitors: a tool identifying new therapeutic targets and side effects.
Blood advances - 9 Jun 2020
Estupiñán H Yesid, Bouderlique Thibault, He Chenfei, Berglöf Anna, Gupta Dhanu, Saher Osama, Daza Cruz Miguel Ángel, Peña-Perez Lucia, Yu Liang, Zain Rula, Karlsson Mikael C I, Månsson Robert, Smith C I Edvard
Abstract excerpt
Pharmacological inhibitors of Bruton tyrosine kinase (BTK) have revolutionized treatment of B-lymphocyte malignancies and show great promise for dampening autoimmunity. The predominant BTK inhibitors tether irreversibly by covalently binding to cysteine 481 in the BTK catalytic domain. Substitution of cysteine 481 for serine (C481S) is the most common mechanism for acquired drug resistance. We generated a novel...
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