Receptor tyrosine kinases (RTKs), are the most successful class for drug target among the 518 known kinases. Receptors tyrosine kinases (RTKs) regulate a broad range of cellular functions, including proliferation, differentiation, survival, and apoptosis and have been intensively studied in development and cancer.
Targeting of Receptor tyrosine kinases (RTKs) has resulted in many marketed small molecule and antibody-based drugs in a number of different solid tumors and hematological malignancies, and more recently in inflammatory diseases such as idiopathic pulmonary fibrosis.
In addition, receptor tyrosine kinases (RTKs) are a very important class of oncology drug targets with >20 small molecule kinase inhibitors already FDA-approved for various cancer treatments, and a large number of kinase inhibitors are currently under various stages of clinic trials.
| Category | Drug Target | HGNC-approved name |
|---|---|---|
| AXL receptor family | AXL | AXL receptor tyrosine kinase |
| Colony-stimulating factor/CSF receptor | CSF1R | Colony-stimulating factor 1 receptor |
| Discoidin domain receptor/DDR family | DDR1 DDR2 |
Discoidin domain receptor tyrosine kinase 1 Discoidin domain receptor tyrosine kinase 2 |
| EPH receptor family | EPHA1 EPHA2 EPHA3 EPHA4 EPHA5 EPHA6 EPHA7 EPHA8 EPHA9 EPHA10 EPHB1 EPHB2 EPHB3 EPHB4 EPHB6 |
EPH receptor A1 EPH receptor A2 EPH receptor A3 EPH receptor A4 EPH receptor A5 EPH receptor A6 EPH receptor A7 EPH receptor A8 EPH receptor A9 EPH receptor A10 EPH receptor B1 EPH receptor B2 EPH receptor B3 EPH receptor B4 EPH receptor B6 |
| Epidermal growth factor/EGF receptor family | EGFR ERBB2 ERBB3 ERBB4 |
Epidermal growth factor receptor v-erb-b2 avian erythroblastic leukemia viral oncogene homolog 2 v-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3 v-erb-b2 avian erythroblastic leukemia viral oncogene homolog 4 |
| Fibroblast growth factor/FGF receptor family | FGFR1 FGFR2 FGFR3 FGFR4 |
Fibroblast growth factor receptor 1 Fibroblast growth factor receptor 2 Fibroblast growth factor receptor 3 Fibroblast growth factor receptor 4 |
| Vascular endothelial growth factor/VEGF receptor family | FLT1 KDR FLT3 FLT4 |
fms-related tyrosine kinase 1 Kinase insert domain receptor (a type III receptor tyrosine kinase) fms-related tyrosine kinase 3 fms-related tyrosine kinase 4 |
| Insulin-like growth factor receptor family | IGF1R | Insulin-like growth factor 1 receptor |
| Insulin receptor family | IGF1R | Insulin receptor |
| ALK/LTK receptor family | LTK | Leukocyte receptor tyrosine kinase |
| Trk receptor family | NTRK1 NTRK2 NTRK3 |
Neurotrophic tyrosine kinase, receptor, type 1 Neurotrophic tyrosine kinase, receptor, type 2 Neurotrophic tyrosine kinase, receptor, type 3 |
| MuSK receptor family | MUSK | Muscle, skeletal, receptor tyrosine kinase |
| PDGF receptor family | PDGFRA PDGFRB |
Platelet-derived growth factor receptor, alpha polypeptide Platelet-derived growth factor receptor, beta polypeptide |
| RET receptor family | RET | RET proto-oncogene |
| ROR receptor family | ROR1 ROR2 |
Receptor tyrosine kinase-like orphan receptor 1 Receptor tyrosine kinase-like orphan receptor 2 |
| TIE receptor family | TIE1 TEK |
Tyrosine kinase with immunoglobulin-like and EGF-like domains 1 TEK tyrosine kinase, endothelial |
| Other receptor tyrosine kinases/RTKs tyrofamily | KIT MST1R RYK |
KIT proto-oncogene receptor tyrosine kinase Macrophage-stimulating 1 receptor (c-met-related tyrosine kinase) Receptor-like tyrosine kinase |
1. LaVallee T M, et al. Emerging Receptor Tyrosine Kinase Drug Targets: Implications for Antibody-Based Therapies for Oncology and Immunologic Disorders[J]. Critical Reviews™ in Oncogenesis, 2015, 20(5-6).
2. Bennasroune A, et al. Tyrosine kinase receptors as attractive targets of cancer therapy[J]. Critical reviews in oncology/hematology, 2004, 50(1): 23-38.
