Table 1.
The expression and biological functions of proteins with ibrutinib binding sites
| Proteins | Expression | Biological function | Binding of ibrutinib IC50 (nm) 15 |
|---|---|---|---|
| TEC family kinases | |||
| BTK | B cells, platelets, erythrocytes, macrophages, neutrophils, mast cells, dendritic cells, NK cells 27, 28 | TEC family kinases, non‐receptor tyrosine kinases playing an important role in signalling pathways in hematopoietic cells 29 | 0.5 |
| TEC | B cells, T cells, platelets, erythrocytes, macrophages, neutrophils, mast cells, liver, heart 27, 29, 30 | 78 | |
| ITK | T cells, NK cells, mast cells 27 | 10.7 | |
| BMX | Macrophages, neutrophils, endothelial cells, arterial endothelium 27, 31 | 0.8 | |
| RLK/TXK | T cells, NK cells, mast cells 27, 29, 32 | Not reported | |
| Other kinases | |||
| BLK | B cells, thymocytes, plasmacytoid dendritic cells 16, 33 | Non‐receptor tyrosine kinase of the SRC‐family kinases, involved in B‐lymphocyte development, differentiation and signalling 16 | 0.5 |
| EGFR | Epithelial cells 34 | Epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases involved in cell growth, proliferation and differentiation 34 | 5.6 |
| ErbB2/HER2 | 9.4 | ||
| ErbB4/HER4 | Not reported | ||
| JAK3 | B cells, T cells, NK cells, myeloid cells, vascular smooth muscle cells, endothelium 35 | Janus family of kinases, involved in cytokine receptor‐mediated intracellular signal transduction, cell proliferation and differentiation 35 | 16.1 |