Receptor Tyrosine Kinases/RTKs as Drug Target

Receptors Tyrosine Kinases/RTKs as Drug Target Background

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.

Receptor Tyrosine Kinases/RTKs as Drug Target List

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

Non-Receptor Tyrosine Kinases as Drug Target List

Drug target HGNC-approved name
ABL1 c-abl oncogene 1, non-receptor tyrosine kinase
BMX BMX non-receptor tyrosine kinase
TNK2 Tyrosine kinase, non-receptor, 2

References

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.

Receptors
Receptors Classification
Receptors by Differentiation Cells
Receptors by Drug Target
GPCRs as Drug Target
GPCR Ligands as Drug Target
Nuclear Hormone Receptors as Drug Target
Cell Adhesion Receptors as Drug Target
Host Defense Receptors as Drug Target
Enzyme-Linked Receptors as Drug Target+
- Receptor Tyrosine Kinases as Drug Target
- Receptor Serine/Threonine Kinases as Drug Target
- Receptor Tyrosine Phosphatases as Drug Target
Other Receptors as Drug Target
Receptors by Functions
Receptors Reagent Products
Receptors by Species