Article
Inhibition of Btk by Btk-specific concentrations of ibrutinib and acalabrutinib delays but does not block platelet aggregation mediated by glycoprotein VI.
Haematologica - 1 Dec 2018
Nicolson Phillip L R, Hughes Craig E, Watson Stephanie, Nock Sophie H, Hardy Alexander T, Watson Callum N, Montague Samantha J, Clifford Hayley, Huissoon Aarnoud P, Malcor Jean-Daniel, Thomas Mark R, Pollitt Alice Y, Tomlinson Michael G, Pratt Guy, Watson Steve P
Abstract excerpt
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...
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