isoDGR-Peptides for Integrin Targeting: Is the Time Up for RGD?

Journal of Medicinal Chemistry
Carsten Höltke

Abstract

Integrins are the main cell adhesion mediators on the cell surface. Especially integrin αvβ3 has gained a lot of attention as a target in cancer therapy because it mediates diverse angiogenic processes during tumor development. The peptide sequence Arg-Gly-Asp (RGD), which is present in a number of endogenous integrin ligands like fibronectin, vitronectin, and related proteins of the extracellular matrix (ECM), has been extensively used as a targeting vector for therapeutic as well as diagnostic purposes, and cilengitide, a cyclic RGD peptide, has entered clinical trials for the treatment of various cancers. However, recent advancements utilizing isoDGR, a sequence that was found in aged fibronectin, already show that RGD-based targeting is not the end of the line. Novel developments and a closer investigation of the binding mode of these peptides now show promising results for the future use of such compounds.

References

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Citations

Jan 7, 2019·Toxicon : Official Journal of the International Society on Toxinology·Meire C AlmeidaDebora A Higuchi
Jun 13, 2021·Bioorganic & Medicinal Chemistry·Ozlem Ozen KarakusShaker A Mousa
Dec 4, 2021·Journal of Peptide Science : an Official Publication of the European Peptide Society·Diego A T PiresCarlos Bloch

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