General tumor-associated receptors (TARs)

General tumor-associated receptors (TARs) represent a broad category of cell-surface proteins, including receptors, adhesion molecules, and enzymes, that are significantly overexpressed or mutated in malignant cells compared to healthy tissues (Boonstra et al., 2014). This group encompasses well-known therapeutic targets such as the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and epithelial cell adhesion molecule (EpCAM), which are critical drivers of tumor growth and survival (NIH, 2014). These receptors function by activating key intracellular signaling pathways that promote uncontrolled cell proliferation, angiogenesis, and the evasion of apoptosis. Due to their differential expression, they serve as primary targets for a variety of interventions, including monoclonal antibodies like cetuximab and trastuzumab, as well as small-molecule inhibitors and antibody-drug conjugates (PubChem, 2024; StatPearls, 2023). Beyond therapy, these receptors are utilized as biomarkers for patient stratification and as targets for molecular imaging to visualize tumor margins and metastases. However, the clinical utility of targeting TARs is often challenged by the heterogeneity of expression within tumors and the potential for 'on-target, off-tumor' toxicities when these proteins are present on normal cells.

Other names

Tumor-associated receptorsTumor-associated antigensCancer-associated receptorsTumor-surface markersTumor-associated membrane proteins

Inhibition of ligand binding, inhibition of intracellular tyrosine kinase activity, induction of antibody-dependent cellular cytotoxicity (ADCC), and delivery of cytotoxic payloads or imaging agents via conjugation.