The Potential Use of Peptides in Cancer Treatment

Curr Protein Pept Sci. 2018;19(8):759-770. doi: 10.2174/1389203719666180111150008.


Conventional chemotherapeutic drugs have significant limitations. For example, tumors may develop resistance, cancers may relapse after treatment, and the drugs may induce secondary malignancies in the treatment of metastatic cancer. There is still a great need for drugs that are able to destroy cancer cells selectively, that is, to effectively treat slow-growing and dormant cells without being affected by chemoresistance mechanisms. A growing number of studies indicate that peptides may be beneficial for drug discovery and development. Peptides offer minimal immunogenicity, excellent tissue penetrability, low-cost manufacturability, and ease of modification for enhancing in vivo stability and biological activity, properties which make them ideal candidates for cancer treatment. This review highlights recent advances in and future prospects for the application of peptides as therapeutic agents for cancer therapy. We discuss the application of peptides in cancer therapy, alone and in combination with other peptides or small-molecule chemotherapeutic drugs, for use in targeted cancer therapy. Furthermore, we consider the use of peptides as a carrier for targeted molecular imaging in the diagnosis and follow-up treatment of cancer. This account also reviews the challenges of using peptide drugs and ways to overcome these limitations. The results obtained in studies presented in this paper indicate that peptides are promising candidates for targeted cancer therapy.

Keywords: Cationic antimicrobial peptides; cell-penetrating peptides; chimeric peptide; peptide-drug conjugates; targeted cancer therapy; tumor homing peptides..

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Drug Carriers / chemistry
  • Humans
  • Immunotherapy / methods
  • Molecular Targeted Therapy
  • Neoplasms / diagnosis
  • Neoplasms / drug therapy*
  • Peptides / pharmacology*
  • Peptides / therapeutic use


  • Antineoplastic Agents
  • Drug Carriers
  • Peptides