Receptor overexpressed on cancer cell

A receptor overexpressed on a cancer cell is a protein found on the cell surface that is present in significantly higher numbers than in normal, healthy cells (National Cancer Institute, 2023). This overexpression often results from gene amplification or dysregulated transcriptional control, leading to heightened sensitivity to growth factors (Nature Reviews Cancer, 2021). These receptors frequently serve as "oncogenic drivers," activating downstream signaling pathways like PI3K/AKT or MAPK that promote uncontrolled proliferation and survival (Cell, 2019). In oncology, these proteins are primary targets for precision therapies, including monoclonal antibodies, small molecule inhibitors, and antibody-drug conjugates (Journal of Clinical Oncology, 2022). By targeting these specific receptors, clinicians can achieve greater selectivity for malignant cells, although "on-target, off-tumor" toxicity remains a concern if the receptor is expressed at lower levels in vital organs (ACS Pharmacology & Translational Science, 2020). Common examples of such targets include HER2 in breast cancer and EGFR in lung cancer. Because this term describes a general biological phenomenon rather than a specific molecular entity, it represents a broad class of therapeutic targets used in personalized medicine.

Other names

Tumor-associated receptorCancer-specific overexpressed receptorOncogenic surface receptor

Targeted inhibition via competitive ligand binding, prevention of receptor dimerization, or antibody-dependent cellular cytotoxicity (ADCC).