期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 73, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2022.128888
关键词
? ?? 3 integrin; Polycyclic RGD peptides; Adhesion inhibition
资金
- Foundation of Anhui province Department of Education [KJ2020A0114]
- Hefei Normal University [2020rcjj48]
Cyclic arginine-glycine-aspartic (RGD) peptides with specific binding ability to integrin alpha nu beta 3 have been developed for drug delivery, tracing, and imaging in tumor diagnosis and treatment. In this study, a series of polycyclic RGD peptides with dual, tri, and tetra rings were designed and synthesized using sortase A-mediated ligation. In vitro cell adhesion inhibition tests revealed that the tricyclic RGD peptide exhibited outstanding potency and selectivity for alpha nu beta 3 integrin.
Cyclic arginine-glycine-aspartic (RGD) peptides that specifically bind to integrin alpha nu beta 3 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 alpha nu beta 3 integrin.
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