Table 1.
A list of tyrosine kinase inhibitors have been summarized below
| Types of tyrosine kinase | Location in the cell | Examples |
|---|---|---|
| Non-Receptor Tyrosine Kinase (NRTK) | ||
| 1. Abl | Tyrosine-protein kinase ABL1 also known as ABL1 is a protein that, in humans, is encoded by the ABL1 gene located on chromosome 9 | Imatinib, Nilotinib, Ponatinib, Bafetinib |
| 2. Tec | Tec kinase is expressed in hematopoietic, liver, and kidney cells |
There are no known inhibitors of Tec kinase at the present. However, Tec kinase is downregulated by dephosphorylation of PIP3 by phosphatase enzyme SHIP and by SH2-containing tyrosine phosphatase SHP-1 Dasatinib has also been found to inhibit T cell effector functions through Tec family kinase inhibition |
| 3. Src | It sits just inside the cell membrane | Saracatinib, Bosutinib |
| 4. Fer | FER was found in the cytoplasm and in the nucleus, where it was associated with the chromatin fraction | Tamatinib, Crizotinib, Bosutinib |
|
5. Ack (Activated Cdc42-associated kinase) |
Ack is ubiquitously expressed, with highest expression seen in thymus, spleen, and brain | Dasatinib |
| 6. JAK (Janus Kinase) | The JAK family has four main members, JAK1, JAK2, JAK3, and TYK2. JAK3 is only expressed in the bone marrow and lymphatic system, as well as endothelial cells and vascular smooth muscle cells, other members are expressed in almost all tissues | Abrocitinib, baricitinib, delgocitinib, fedratinib, filgotinib, oclacitinib, pacritinib, peficitinib, ruxolitinib, tofacitinib, and upadacitinib |
| 7. Syk (spleen tyrosine kinase) | Syk is primarily expressed in hematopoietic cells, as well as synoviocytes and vascular endothelial cells | Fostamatinib, Entospletinib, Cerdulatinib |
| 8. Csk (C-terminal Src kinase) | Tyrosine-Kinase CSK is mainly present in the cytoplasm, but also found in lipid rafts making cell–cell junction | Dasatinib, Foretinib, Tamatinib |
| Receptor tyrosine kinase (RTK) | ||
| 1. EGFR (epidermal growth factor receptors) | It is a transmembrane protein with approximately equal portions of the receptor localized outside and inside the cell | Gefitinib, Erlotinib, Afatinib, Dacomitinib, and Osimertinib |
| 2. CCK4 (colon carcinoma kinase 4) | Colon carcinoma kinase 4 (CCK-4) mRNA is highly expressed in human lung tissue and at lower levels in the thyroid gland and ovary | |
| 3. ALK (anaplastic lymphoma kinase) | Anaplastic lymphoma kinase (ALK), aka CD246, is a tyrosine kinase receptor encoded by the ALK gene located on chromosome 2p23.2-p23.1 | Ceritinib, Entrectinib |
| 4. VEGFR (vascular endothelial growth factor receptor) | VEGF receptors are located on both the luminal and abluminal sides of the endothelial cells | bevacizumab, sorafenib, sunitinib, nilotinib, pazopanib, and dasatinib |
| 5. DDR (Discoidin domain receptor tyrosine kinase) | DDR is expressed in epithelial cells, particularly in the kidney, lung, gastrointestinal tract, and the brain | Imatinib, Nilotinib, Ponatinib |
| 6. ROR (RTK-like orphan receptor) | Predominantly located in the plasma membrane | |
| 7. PDGFR (platelet-derived growth factor receptors) | PDGFR are expressed in tumor cells and stromal cells of neoplastic tissues | imatinib, linifanib, nintedanib, and sorafenib |
| 8. Eph (Erythropoietin-producing hepatocellular carcinoma) | Eph receptors have also been detected in the lining of the aorta, brachial arch arteries, umbilical vein, and endocardium | Tesevatinib |
| 9. Tie | The tie tyrosine kinase receptors form the only receptor families that are predominantly expressed on endothelial cells | Pexmetinib, Cabozantinib |
| 10. Fak (focal adhesion kinase) | FAK is typically located at structures known as focal adhesions, which are multiprotein structures that link the extracellular matrix (ECM) to the cytoplasmic cytoskeleton | VS-6062, Defactinib |
| 11. Axl | AXL protein is expressed in normal tissues, particularly in bone marrow stroma and myeloid cells, and in tumor cells and tumor vasculature | Foretinib, Cabozantinib, Merestinib |
| 12. Mertk (MER proto-oncogene, tyrosine kinase) | MERTK is highly expressed in monocytes/macrophages, testis, and epithelial cells including the retinal pigment epithelium (RPE) | |