Ontology highlight
ABSTRACT:
SUBMITTER: Nicolson PLR
PROVIDER: S-EPMC6269309 | biostudies-literature | 2018 Dec
REPOSITORIES: biostudies-literature
Nicolson Phillip L R PLR Hughes Craig E CE Watson Stephanie S Nock Sophie H SH Hardy Alexander T AT Watson Callum N CN Montague Samantha J SJ Clifford Hayley H Huissoon Aarnoud P AP Malcor Jean-Daniel JD Thomas Mark R MR Thomas Mark R MR Pollitt Alice Y AY Tomlinson Michael G MG Pratt Guy G Watson Steve P SP
Haematologica 20180719 12
Ibrutinib and acalabrutinib are irreversible inhibitors of Bruton tyrosine kinase used in the treatment of B-cell malignancies. They bind irreversibly to cysteine 481 of Bruton tyrosine kinase, blocking autophosphorylation on tyrosine 223 and phosphorylation of downstream substrates including phospholipase C-γ2. In the present study, we demonstrate that concentrations of ibrutinib and acalabrutinib that block Bruton tyrosine kinase activity, as shown by loss of phosphorylation at tyrosine 223 an ...[more]