New potent and selective αvβ3 integrin ligands: Macrocyclic peptides containing RGD motif synthesized by sortase A-mediated ligation

Three 14-mer macrocyclic peptides containing RGD structure motifs were synthesized by sortase A-mediated head to tail ligation, and their binding affinity to integrin was evaluated by cell-based competition experiments. [Display omitted] Three 14-mer macrocyclic peptides 1–3 containing mono-, di- an...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2017-05, Vol.27 (9), p.1911-1913
Main Authors: Wu, Zhimeng, Cheng, Xiaozhong, Hong, Haofei, Zhao, Xinrui, Zhou, Zhifang
Format: Article
Language:English
Subjects:
Cyclization
Macrocyclic
Peptide
RGD
Sortase A
αvβ3 integrin
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Summary:Three 14-mer macrocyclic peptides containing RGD structure motifs were synthesized by sortase A-mediated head to tail ligation, and their binding affinity to integrin was evaluated by cell-based competition experiments. [Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2017.03.035