01 2019 Organic & biomolecular chemistry

Tuning the properties of a cyclic RGD-containing tetrapeptide through backbone fluorination.


Au C, Gonzalez C, Leung YC, Mansour F, Trinh J, Wang Z, Hu XG, Griffith R, Pasquier E, Hunter L


Stereoselective fluorination is investigated as a method for modulating the properties of a cyclic RGD-containing tetrapeptide. Three key outcomes of fluorination are assessed: (i) the effect on peptide cyclisation efficiency; (ii) the ability to fine-tune the molecular conformation; and (iii) the effect on the cyclic peptides’ biological activity. Fluorination is found to exert pronounced effects against all three criteria.

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