Recent progress in biomedical applications of RGD‐based ligand: From precise cancer theranostics to biomaterial engineering: A systematic review

Abstract

Arginine-glycine-aspartic acid (RGD) peptide family is known as the most prominent ligand for extracellular domain of integrin receptors. Specific expression of these receptors in various tissue of human body and tight association of their expression profile with various pathophysiological conditions made these receptors a suitable targeting candidate for several disease diagnosis and treatment as well as regeneration of various organs. For these reasons, various forms of RGD-based integrins ligands have been greatly used in biomedical studies. Here, we summarized the last decade application progress of RGD for cancer theranostics, control of inflammation, thrombosis inhibition and critically discussed the effect of RGD peptides structure and sequence on the efficacy of gene/drug delivery systems in preclinical studies. Furthermore, we will show recent advances in application of RGD functionalized biomaterials for various tissue regenerations including cornea repair, artificial neovascularization and bone tissue regeneration.Finally, we analyzed clinically translatability of RGD peptides, considering examples of integrin ligands in clinical trials. In conclusion, prospects on using RGD peptide for precise drug delivery and biomaterial engineering are well discussed.

RGD peptide-mediated liposomal curcumin targeted delivery to breast cancer cells

“…27 The Arginine – Glycine – Aspartic acid (RGD) tripeptide has been found to exhibit high-binding affinity toward α v β 3 . 28 , 29 Various RGD-conjugated nano-formulations have been reported for the targeted delivery of chemotherapeutics to breast cancer cells through α v β 3 integrin recognition. 25,26,30 Various techniques exist on the modification of liposomal surface with RGD peptide, a major one is through covalent anchorage using polyethylene glycol (PEG) as a linker.…”

<p>Distinct Proteins in Protein Corona of Nanoparticles Represent a Promising Venue for Endogenous Targeting – Part II: In vitro and in vivo Kinetics Study</p>

“…This is consistent with the previous reports showing a competitive inhibition of NPs' uptake in the presence of RGD peptide in a concentration-dependent manner. 50 In SR conditions, the one-compartment PK analysis was performed using PK solver add-in of Microsoft Excel 2016 in order to have a more accurate comparison of the uptake and the elimination parameters of uNPs and cNPs. The model selection has been justified in the view of the previous studies.…”

“…This is consistent with the previous reports showing a competitive inhibition of NPs' uptake in the presence of RGD peptide in a concentration-dependent manner. 50 …”

<p>Distinct Proteins in Protein Corona of Nanoparticles Represent a Promising Venue for Endogenous Targeting – Part I: In vitro Release and Intracellular Uptake Perspective</p>

“…International Journal of Nanomedicine 2020:15 In the in vitro uptake results, the higher extent of NPs' accumulation upon peptide conjugation, especially for the hybrid formulations (cNP3 and cNP4) could be attributed to both the role of cRDGyk in anchoring the NPs to the integrin receptors bringing about higher accumulation tendencies 24 and the advantage of the lipid coat in increasing the cellular levels of the NPs. 62 This observation could also be related to the zeta potential of cNPs; it was previously discussed in this work (Table 2) that peptide conjugation reduced the overall surface charge of the NPs.…”

“…cRGDyk cyclic pentapeptide is a selective inhibitor to αvβ3 integrins that are cell surface proteins overexpressed in melanoma. [19][20][21][22][23][24] The PC of the synthesized NPs has been characterized in terms of the quantity and the abundance of distinct proteins of interest. The role of this PC on the NPs' behavior in terms of the in vitro release of loaded cargos and the in vitro cellular uptake has then been characterized.…”