Tumor-associated cell surface receptor

Tumor-associated cell surface receptors are a broad category of proteins expressed on the plasma membrane of cancer cells that play pivotal roles in tumor progression and serve as essential targets for precision medicine. These receptors, which include receptor tyrosine kinases (RTKs), G protein-coupled receptors (GPCRs), and various glycoproteins, are often overexpressed or mutated in malignancies, driving pathways associated with uncontrolled cell proliferation, survival, and metastasis [1, 2]. Due to their accessibility on the cell surface, they are targeted by a variety of therapeutic agents, including monoclonal antibodies, bispecific antibodies, and antibody-drug conjugates (ADCs) [3]. These therapies work by blocking oncogenic signaling, recruiting the immune system to destroy the tumor, or delivering toxic payloads directly into the cell. However, the clinical success of targeting these receptors is frequently challenged by "on-target, off-tumor" toxicities in healthy tissues and the emergence of resistance mechanisms such as receptor downregulation or bypass signaling [2, 4].

Other names

Tumor-associated antigenCancer cell surface markerTumor-specific surface proteinCell surface tumor antigen

The mechanisms of action for drugs targeting these receptors include the blockade of ligand binding to inhibit downstream signaling, the prevention of receptor dimerization, the induction of immune-mediated cell killing such as antibody-dependent cellular cytotoxicity (ADCC), and the targeted delivery of cytotoxic payloads via receptor-mediated endocytosis of antibody-drug conjugates [2, 3, 4].