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Mol Pharm. 2012 Nov 5;9(11):2961-73. doi: 10.1021/mp3002733. Epub 2012 Oct 4.

RGD-based strategies to target alpha(v) beta(3) integrin in cancer therapy and diagnosis.

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Université catholique de Louvain, Pharmaceutics and Drug Delivery, Louvain Drug Research Institute, Avenue E. Mounier, 73 B1 73 12, B-1200, Brussels, Belgium.


The integrin α(v)β(3) plays an important role in angiogenesis. It is expressed on tumoral endothelial cells as well as on some tumor cells. RGD peptides are well-known to bind preferentially to the α(v)β(3) integrin. In this context, targeting tumor cells or tumor vasculature by RGD-based strategies is a promising approach for delivering anticancer drugs or contrast agents for cancer therapy and diagnosis. RGD-based strategies include antagonist drugs (peptidic or peptidomimetic) of the RGD sequence, RGD-conjugates, and the grafting of the RGD peptide or peptidomimetic, as targeting ligand, at the surface of nanocarriers. Although all strategies are overviewed, this review aims to particularly highlight the position of RGD-based nanoparticles in cancer therapy and imaging. This review is divided into three parts: the first one describes the context of angiogenesis, the role of the integrin α(v)β(3), and the binding of the RGD peptide to this integrin; the second one focuses on RGD-based strategies in cancer therapy; while the third one focuses on RGD-based strategies in cancer diagnosis.

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