School of Chemistry, UNSW Sydney, NSW 2052, Australia.
Org Biomol Chem. 2019 Jan 16;17(3):664-674. doi: 10.1039/c8ob02679c.
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.
手性选择性氟化被研究作为一种调节含有环状 RGD 的四肽性质的方法。评估了氟化的三个关键结果：（i）对肽环化效率的影响；（ii）精细调整分子构象的能力；和（iii）对环状肽生物活性的影响。发现氟化对所有三个标准都有显著影响。
