Table 1 Classes of selected kinase inhibitors26,28.
Class | Mechanism of action | Examples |
|---|---|---|
Type I | Binding in the ATP-binding pocket of the active conformation of the enzyme (DFG-in and αC-helix-in) | cabozantinib, ceritinib, gefitinib, palbociclib, pazopanib, ponatinib, ruxolitinib, tofacitinib |
Type I1/2 Type II | Binding in the ATP-binding pocket of the inactive conformation of the enzyme (type I1/2: DFG-Asp in; type II: DFG-Asp out) | dasatinib, imatinib, lapatinib, lenvatinib, nilotinib, regorafenib, sorafenib, sunitinib, vemurafenib |
Type III Type IV | Allosteric inhibitors binding to a site in the kinase domain either next to the ATP-binding pocket or remote from the ATP-binding pocket | trametinib, everolimus, sirolimus, temsirolimus |
Type V | Bivalent inhibitors that bind two different portions of the kinase lobe | lenvatinib28 |
Type VI | Covalent inhibitors | afatinib, ibrutinib |
