Unlocking the potential of tumor-targeting peptides in precision oncology

Targeted cancer therapy has emerged as a promising alternative to conventional chemotherapy, which is often plagued by poor selectivity, off-target effects, and drug resistance. Among the various targeting agents in development, peptides stand out for their unique advantages, including minimal immunogenicity, high tissue penetration, and ease of modification. Their small size, specificity, and flexibility allow them to target cancer cells while minimizing damage to healthy tissue selectively. Peptide-based therapies have shown great potential in enhancing the efficacy of drug delivery, improving tumor imaging, and reducing adverse effects. With cancer responsible for millions of deaths worldwide, the development of peptide-based therapeutics offers new hope in addressing the limitations of current treatments. As detailed studies on different aspects of targeting peptides are crucial for optimizing drug development, this review provides a comprehensive overview of the literature on tumor-targeting peptides, including their structure, sources, modes of action, and their application in cancer therapy—both as standalone agents and in fusion drugs. Additionally, various computational tools for peptide-based tumor-targeting drug design and validation are explored. The promising results from these studies highlight peptides as ideal candidates for targeted cancer therapies, offering valuable insights for researchers and accelerating the discovery of novel anti-tumor peptide base drug candidates.