Number of common targets | Target | Imatinib | Dasatinib | Nilotinib | Bosutinib | Ponatinib |
All | ||||||
ABL | ✓ | ✓ | ✓ | ✓ | ✓ | |
4 | ||||||
Kit | ✓ | ✓ | ✓ | ✓ | ||
PDGFRA | ✓ | ✓ | ✓ | ✓ | ||
PDGFRB | ✓ | ✓ | ✓ | ✓ | ||
DDR1 | ✓ | ✓ | ✓ | ✓ | ||
CSF1R | ✓ | ✓ | ✓ | ✓ | ||
LCK | ✓ | ✓ | ✓ | ✓ | ||
EGFR | ✓ | ✓ | ✓ | ✓ | ||
3 | ||||||
RET | ✓ | ✓ | ✓ | |||
FYN | ✓ | ✓ | ✓ | |||
SRC | ✓ | ✓ | ✓ | |||
YES1 | ✓ | ✓ | ✓ | |||
LYN | ✓ | ✓ | ✓ | |||
HCK | ✓ | ✓ | ✓ | |||
NTRK1 | ✓ | ✓ | ✓ | |||
2 | ||||||
CA1,2,9,12 | ✓ | ✓ | ||||
AKT1 | ✓ | ✓ | ||||
CSK | ✓ | ✓ | ||||
TNK2 | ✓ | ✓ | ||||
BTK | ✓ | ✓ | ||||
SYK | ✓ | ✓ | ||||
FLT3 | ✓ | ✓ | ||||
EPHA2 | ✓ | ✓ | ||||
EPHA5 | ✓ | ✓ | ||||
EPHB1 | ✓ | ✓ | ||||
FGFR1,2 | ✓ | ✓ | ||||
EPHB4 | ✓ | ✓ | ||||
PTK2B | ✓ | ✓ | ||||
None | ||||||
ACVR1B | ✓ | |||||
ACVRL1 | ✓ | |||||
ACVR1 | ✓ | |||||
TUBA1A | ✓ | |||||
MAPK14 | ✓ | |||||
FGFR3,4 | ✓ | |||||
VEGFR1,2,3 | ✓ |
Number of targets ranges from seven (nilotinib) to 29 (dasatinib). 28 targets are common to at least two TKIs. Among those, tyrosine-protein kinase ABL is systematically reported explaining their benefit in CML. Targets were extracted from Supertarget Database (http://insilico.charite.de/supertarget/index.php) and article by Greuber et al. [13]. Each tick signifies inhibition by the TKI in the corresponding column. ABL: abelson murine leukaemia viral oncogene; PDGFRA: platelet-derived growth factor receptor A; PFGFRB: platelet-derived growth factor receptor B; DDR1: discoidin domain receptor 1; CSF1R: colony stimulating factor 1 receptor; LCK: lymphocyte cell-specific kinase; EGFR: epidermal growth factor receptor; HCK: haemopoeitic cell kinase; NTRK1: neurotrophic tyrosine receptor kinase 1; CSK: C-terminal src kinase; TNK2: tyrosine kinases non-receptor 2; BTK: Bruton's tyrosine kinase; SYK: spleen tyrosine kinase; FLT3: fms-like tyrosine kinase 3; EPHA2: ephrin type A receptor 2; EPHA5: ephrin type A receptor 5; EPHB1: ephrin type B receptor 1; FGFR: fibroblast growth factor receptor; EPHB 4: ephrin type B receptor 4; PTK2B: protein tyrosine kinase 2 beta; ACVR1B: activin receptor type-1B; ACVRL1: activin receptor like type 1; ACVR1: activin receptor type 1; TUBA1A: tubulin alpha-1A; MAPK14: mitogen-activated protein kinase 14; FGFR: fibroblast growth factor receptor; VEGFR: vascular endothelial growth factor receptor.