Internalizing RGD, a great motif for targeted peptide and protein delivery: a review article

Drug Deliv Transl Res. 2022 Oct;12(10):2261-2274. doi: 10.1007/s13346-022-01116-7. Epub 2022 Jan 11.

Abstract

Understanding that cancer is one of the most important health problems, especially in advanced societies, is not difficult. The term of targeted cancer therapy has also been well known as an ideal treatment strategy in the recent years. Peptides with ability to specifically recognize the cancer cells with suitable penetration properties have been used as the targeting motif in this regard. In the present review article, we focus on an individual RGD-derived peptide with ability to recognize the integrin receptor on the cancer cell surface like its ancestor with an additional outstanding feature to penetrate to extravascular space of tumor and ability to penetrate to cancer cells unlike the original peptide. This peptide which has been named "internalizing RGD" or "iRGD" has been the focus of researches as a new targeting motif since it was discovered. To date, many types of molecules have been associated with this peptide for their targeted delivery to cancer cells. In this review article, we have discussed a summary of penetration mechanisms of iRGD and all introduced peptides and proteins attached to this attractive cell-penetrating peptide and have expressed the results of the studies.

Keywords: Cancer; Internalizing RGD; Penetration; Targeted therapy.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cell-Penetrating Peptides*
  • Oligopeptides* / chemistry

Substances

  • Cell-Penetrating Peptides
  • Oligopeptides