Target intelligence / Profile preview

Tyrosine-protein kinase EphA3 (EphA3)

Target
EphA3
Molecular classification
Receptor, Enzyme, Receptor tyrosine kinase (RTK), Membrane receptor
01

Overview

Tyrosine-protein kinase EphA3 is a receptor tyrosine kinase belonging to the ephrin receptor subfamily, encoded by the EPHA3 gene located on chromosome 3p11.2. The receptor has an extracellular region with a cysteine-rich domain and fibronectin type III repeats, a transmembrane region, and an intracellular tyrosine kinase domain. EphA3 primarily binds ephrin-A family ligands, mediating repulsive and adhesive cell signaling important in embryonic tissue patterning, cell positioning, and nervous system development. In adults, EphA3 is sparsely expressed in most tissues but is overexpressed in various malignancies, making it a therapeutic target for cancer drug development, particularly monoclonal antibodies and kinase inhibitors[5][12][13][16][15][14].

Other names
EPH receptor A3EPHA3EK4ETKHEKETK1HEK4TYRO4Ephrin type-A receptor 3EPH-like kinase 4Eph-like tyrosine kinase 1Human embryo kinaseHuman embryo kinase 1Mek4rEK4TYRO4 protein tyrosine kinaseTyrosine-protein kinase receptor ETK1Tyrosine-protein kinase receptor REK4Tyrosine-protein kinase TYRO4testicular tissue protein Li 64AW492086End3I79_002835[5][12]
02

Mechanism of action

Inhibition of kinase activity Disruption of ligand (ephrin) binding Modulation of cell signaling to inhibit tumor cell migration, proliferation, and survival Antibody-dependent cellular cytotoxicity (for some monoclonal antibodies)

03

Biological functions

Signal transductionRegulation of cell adhesionRegulation of cell migrationCell proliferationNervous system developmentCell differentiationApoptosis (anti-apoptotic ability)
04

Disease associations

Cancer (various tumors, including leukemia and solid malignancies)Neurodevelopmental disorders (due to its role in the nervous system)
05

Safety considerations

Potential off-target effects due to EphA3 expression in some normal adult tissuesUnknown long-term effects of sustained inhibition in humans (based on limited trial data)
06

Interacting drugs

Drug candidates are in preclinical and early-phase trials; specific named, marketed drugs directly targeting EphA3 in humans are not established as of current literature, but monoclonal antibodies (e.g., KB004) have entered clinical trials for cancer therapy[15].
07

Biomarkers

EphA3 protein expression (biomarker for certain cancers, such as acute lymphoblastic leukemia and other solid tumors)[15][16]

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