Molecular Pharmaceutics· 2012Q1· Review
RGD-Based Strategies To Target Alpha(v) Beta(3) Integrin in Cancer Therapy and Diagnosis
- 943citations
- Q1SCImago
- 2012year
Short summary
RGD peptides can selectively bind to the alpha(v)beta(3) integrin, a key molecule in tumor angiogenesis and expressed on tumor cells. This review highlights RGD-based strategies, particularly nanoparticles, for targeted cancer therapy and diagnosis.
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Key points
- Alpha(v)beta(3) integrin is a targetable marker for cancer therapy and diagnosis.
- RGD peptides exhibit preferential binding to alpha(v)beta(3) integrin.
- RGD-based strategies include antagonist drugs, conjugates, and RGD-modified nanocarriers.
- RGD-based nanoparticles are particularly emphasized for cancer therapy and imaging.
AI-generated from the title and abstract; the full text is not read.
Abstract
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.
The authors' abstract, as published at the source. Molecular Pharmaceutics, 2012 · DOI ↗
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Field: Immunology and Allergy
Immunology and AllergyMedicine