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Preparing a 68Ga-labeled Arginine Glycine Aspartate RGD-peptide for Angiogenesis
Published on: January 7, 2019
Sortase A-mediated cyclization of novel polycyclic RGD peptides for ανβ3 integrin targeting
Yajun Chen1, Lixuan Jia1, Guilan Zhu1
1Anhui Engineering Laboratory for Medicinal and Food Homologous Natural Resources Exploration, Hefei Normal University, Hefei 230601, China.
Abstract:
Cyclic arginine-glycine-aspartic (RGD) peptides that specifically bind to integrin ανβ3 have been developed for drug delivery, tracers, and imaging for tumor diagnosis and treatment. Herein, a series of polycyclic RGD peptides containing dual, tri, and tetra rings were designed and synthesized through sortase A-mediated ligation. An in vitro test on cell adhesion inhibition indicated that the RGD peptide containing tricylic structure exhibited outstanding potency and selectivity for ανβ3 integrin.
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