Sortase A-mediated cyclization of novel polycyclic RGD peptides for ανβ3 integrin targeting.

Yajun Chen, Lixuan Jia, Guilan Zhu, Wei Wang, Ming Geng, Hongxia Lu, Yan Zhang, Minghui Zhou, Fangyan Zhang, Xiaozhong Cheng

Bioorganic & medicinal chemistry letters 2022 Oct 01

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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. Copyright © 2022 Elsevier Ltd. All rights reserved.

Citation

Yajun Chen, Lixuan Jia, Guilan Zhu, Wei Wang, Ming Geng, Hongxia Lu, Yan Zhang, Minghui Zhou, Fangyan Zhang, Xiaozhong Cheng. Sortase A-mediated cyclization of novel polycyclic RGD peptides for ανβ3 integrin targeting. Bioorganic & medicinal chemistry letters. 2022 Oct 01;73:128888