Journal
THERANOSTICS
Volume 1, Issue -, Pages 189-200Publisher
IVYSPRING INT PUBL
DOI: 10.7150/thno/v01p0189
Keywords
Integrin; Targeted delivery; Chemotherapeutics; RGD; Bioconjugation
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Funding
- National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health (NIH)
- NATIONAL INSTITUTE OF BIOMEDICAL IMAGING AND BIOENGINEERING [ZIAEB000073] Funding Source: NIH RePORTER
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Targeted delivery of chemotherapeutics is defined in the sense, that is, to maximize the therapeutic index of a chemotherapeutic agent by strictly localizing its pharmacological activity to the site or tissue of action. Integrins are a family of heterodimeric transmembrane glycoproteins involved in a wide range of cell-to-extracellular matrix (ECM) and cell-to-cell interactions. As cell surface receptors, integrins readily interact with extracellular ligands and play a vital role in angiogenesis, leukocytes function and tumor development, which sets up integrins as an excellent target for chemotherapy treatment. The peptide ligands containing the arginine-glycine-aspartic acid (RGD), which displays a strong binding affinity and selectivity to integrins, particularly to integrin alpha v beta 3, have been developed to conjugate with various conventional chemotherapeutic agents, such as small molecules, peptides and proteins, and nanoparticle-carried drugs for integtrin targeted therapeutic studies. This review highlights the recent advances in integrin targeted delivery of chemotherapeutic agents with emphasis on target of integrin alpha v beta 3, and describes the considerations for the design of the diverse RGD peptide-chemotherapeutics conjugates and their major applications.
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