Journal
CURRENT MEDICINAL CHEMISTRY
Volume 17, Issue 13, Pages 1255-1299Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986710790936301
Keywords
Integrins; design of RGD ligands; cancer therapy and imaging; targeted drug delivery; multimodality; integrin targeted nanoparticles
Funding
- University of Milan, Italy
- Regione Autonoma della Sardegna
- Ministero dell'Istruzione, dell'Universa e della Ricerca
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The outstanding physio-pathological role played by integrin receptors in living subjects motivates the enormous interest shown by scientists worldwide for this topic. More than twenty years of research has spanned across the structural and functional elucidation of these proteins and over their antagonism-based biomedical applications. The proof-of-concept stage, aimed at identifying potent inhibitors, covered a decade of studies, and paved the way for a more advanced era of research where these antagonist molecules were thrown into the deep end of applicative studies. This review intends to summarize the major efforts conducted thus far and focuses on the design, synthesis and biomedical applications of cyclic RGD-containing alpha(v)beta(3) integrin antagonists, in both their small and macromolecular formats. In particular, Chapters 1 and 2 offer a comprehensive outlook on the rational basis for the design of integrin inhibitors, Chapter 3 chronicles the biological and medical applications of monofunctional RGD integrin ligands both in their monomeric and multimeric asset, and Chapter 4 illustrates the potential of RGD-based multifunctional systems in molecular medicine.
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