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New potent and selective αvβ3 integrin ligands: Macrocyclic peptides containing RGD motif synthesized by sortase
Zhimeng Wu1, Xiaozhong Cheng1, Haofei Hong1
1Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
Bioorganic & Medicinal Chemistry Letters
|March 30, 2017
Abstract:
Three 14-mer macrocyclic peptides 1-3 containing mono-, di- and tri-RGD structure motif were designed and synthesized by sortase A-mediated ligation in good yields. The results of in intro cell-based biological assays indicated that linear peptide 5 and macrocyclic peptide 1, containing di-RGD and mono-RGD motif respectively, showed remarkable potency and selectivity to αvβ3 integrin.

