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Varna Medical Forum

Aspects Of The Use Of RGD Peptides

Momchil Lambev, Antonia Hristova, Dimana Dimitrova, Silvia Mihaylova, Stefka Valcheva-Kuzmanova, Tamara Pajpanova

Abstract

The amino acid sequence L-argininyl-glycyl-L-asparaginic acid (RGD) is inherent in many extracellular and intracellular proteins. Initially, the RGD peptide was identified in fibronectin in 1984 by E. Ruoslahti, who found that these three amino acids were the site of adhesion of cells to the extracellular matrix or other cells by cell adhesion molecules as integrins. Subsequently, this tri-amino acid residue was also found in many other proteins in the extracellular matrix and blood. It is a common pattern of recognition by some cell receptors. Following the discovery of the RGD sequence as a potential ligand for binding to cellular integrins (most commonly αvβ3), RGD-mediated small molecules and RGD-containing therapeutic peptides and proteins have been used for controlled drug distribution and as agents for cell targeting and endosomal delivery. Due to the large number of integrins in endothelial cells and blood vessels to tumor tissues, RGD-mediated drug delivery is of a particular interest in cancer therapy. Furthermore, the RGD-integrin system is used for target cell recognition and internalization, which is applied to human-created structures that mimic pathogens. Because of this, the systems are being tested for use as diagnostics, therapeutics, and regenerating transplanted tissues.

The detection of tumors is characterized by high specificity and sensitivity by conjugation of markers with RGD peptides. This important technology is widely used for early diagnosis and differential diagnosis of tumors as well as for clinical analysis and treatment. RGD-modified drugs and imaging agents have been created by conjugation of RGD peptides to carriers. The carrier molecules are loaded with drug molecules or signal-generating molecules. RGD peptides and RGD mimetics are also applied to modify liposomes, polymers and peptides in a chemical way that increases their biological effects as therapeutic agents.

RGD peptides are promising molecules with great future use in therapy as a drug-delivery system, in imaging diagnostics and in tissue engineering.


Keywords

RGD peptides; anticancer therapy; drug delivery; imaging diagnostics; tissue engineering

Full Text


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DOI: http://dx.doi.org/10.14748/vmf.v7i0.6107

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