PSMA-targeting linkers are chemical bridges that connect a PSMA-binding molecule, such as a ligand or antibody, to therapeutic or diagnostic payloads for selective delivery to PSMA-expressing cancer cells. They play a critical role in the efficacy and safety of PSMA-targeted agents by ensuring precise payload release at the tumor site. Linker design-considering length, flexibility, stability, and chemical composition-affects binding affinity, biodistribution, and pharmacological performance. Common types include enzyme-cleavable peptide linkers (e.g., valine-citrulline), aliphatic chains for structural spacing, and linkers incorporating charged groups to enhance tumor uptake, optimize targeting efficiency, and minimize off-target effects.