title: New potent and selective αvβ3integrin ligands: Macrocyclic peptides containing RGD motif synthesized by sortase A-mediated ligation.
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 αvβ3integrin.
authors.affiliation: Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China. Electronic address: zwu@jiangnan.edu.cn.
authors.forename: Zhimeng
authors.initials: Z
authors.lastname: Wu
authors.affiliation: Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
authors.forename: Xiaozhong
authors.initials: X
authors.lastname: Cheng
authors.affiliation: Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
authors.forename: Haofei
authors.initials: H
authors.lastname: Hong
authors.affiliation: Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
authors.forename: Xinrui
authors.initials: X
authors.lastname: Zhao
authors.affiliation: Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
authors.forename: Zhifang
authors.initials: Z
authors.lastname: Zhou
mesh_terms: D019881:Aminoacyltransferases / Q000378:metabolism; D001426:Bacterial Proteins / Q000378:metabolism; D001483:Base Sequence; D002448:Cell Adhesion / Q000187:drug effects; D002460:Cell Line; D003500:Cyclization; D003546:Cysteine Endopeptidases / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D047028:Macrocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000201:enzymology
chemical_list: D001426:Bacterial Proteins; D039302:Integrin alphaVbeta3; D047028:Macrocyclic Compounds; D009842:Oligopeptides; D010455:Peptides; D010456:Peptides, Cyclic; C047981:arginyl-glycyl-aspartic acid; D019881:Aminoacyltransferases; C120542:sortase A; D003546:Cysteine Endopeptidases
keywords: Cyclization; Macrocyclic; Peptide; RGD; Sortase A; αvβ(3) integrin