Issue 3, 2019

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

Abstract

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.

Graphical abstract: Tuning the properties of a cyclic RGD-containing tetrapeptide through backbone fluorination

Supplementary files

Article information

Article type
Paper
Submitted
30 Oct 2018
Accepted
14 Dec 2018
First published
14 Dec 2018

Org. Biomol. Chem., 2019,17, 664-674

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

C. Au, C. Gonzalez, Y. C. Leung, F. Mansour, J. Trinh, Z. Wang, X. Hu, R. Griffith, E. Pasquier and L. Hunter, Org. Biomol. Chem., 2019, 17, 664 DOI: 10.1039/C8OB02679C

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