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Cyclic RGD and isoDGR Integrin Ligands Containing cis-2-amino-1-cyclopentanecarboxylic (cis-β-ACPC) Scaffolds

Panzeri, Silvia ; Arosio, Daniela ; Gazzola, Silvia ; Belvisi, Laura ; Civera, Monica ; Potenza, Donatella ; Vasile, Francesca ; Kemker, Isabell ; Ertl, Thomas ; Sewald, Norbert ; Reiser, Oliver ; Piarulli, Umberto



Abstract

Integrin ligands containing the tripeptide sequences Arg-Gly-Asp (RGD) and iso-Asp-Gly- Arg (isoDGR) were actively investigated as inhibitors of tumor angiogenesis and directing unit in tumor-targeting drug conjugates. Reported herein is the synthesis, of two RGD and one isoDGR cyclic peptidomimetics containing (1S,2R) and (1R,2S) cis-2-amino-1-cyclopentanecarboxylic acid (cis-beta-ACPC), using a ...

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