Recent advances in the tumor-penetrating peptide internalizing RGD for cancer treatment and diagnosis.

Abstract

Cancer has become a prominent disease that seriously endangers human health. The complexity of the biological characteristics of the tumor makes it challenging for traditional therapeutic drugs to penetrate tumor tissues and exert their antitumor effects. Internalizing RGD peptide (iRGD) is a novel tumor-homing peptide that binds to αvβ3 and αvβ5 integrins on the surface of tumor vessels through the C-end rule (CendR) motif. The CendR motif binds to the neuropilin-1 (NRP-1) receptor on tumor cells, initiating NRP-1-mediated transcytosis to facilitate drug entry into the tumor tissue. Multiple studies demonstrated that iRGD improved the penetration and targeting of antitumor drugs, thereby enhancing their antitumor efficacy. In this review, we initially described the origins of iRGD and its penetration mechanism. Furthermore, we presented updates on the application of iRGD in cancer chemotherapy, photodynamic therapy, gene therapy, immunotherapy, treatment with antibodies or protein-based biologics, and tumor imaging.

• Authors: Jing Qian, Sheng Zhou, Peng Lin, Jin Lei, Shiqi Zheng, Wenmang Xu, Yuanyuan Wang, Ziran Gao, Julun Yang
• Journal: Drug development research (Drug Dev Res) Vol. 84 Issue 4 Pg. 654-670 (Jun 2023) ISSN: 1098-2299 [Electronic] United States
• PMID: 36959702 (Publication Type: Journal Article, Review)
• Copyright: © 2023 Wiley Periodicals LLC.

Chemical References

• Peptides
• Antineoplastic Agents
• Oligopeptides

Topics

• Humans
• Cell Line, Tumor
• Peptides
• Antineoplastic Agents (therapeutic use)
• Oligopeptides (therapeutic use)
• Drug Delivery Systems (methods)
• Neoplasms (diagnostic imaging, drug therapy)