title: Switching substitution groups on the in-tether chiral centre influences backbone peptides' permeability and target binding affinity.
abstract: Different substitution groups on the in-tether chiral centre of chirality-induced helical peptides (CIH peptides) showed distinguishable effects on the peptides' cellular uptakes and binding affinities with the estrogen receptor α(ER-α). This study proves that in-tether chiral centres are a valuable modification site for constructing peptide ligands with preferable biophysical properties.
authors.affiliation: School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055, China. lizg@pkusz.edu.cn.
authors.forename: Yixiang
authors.initials: Y
authors.lastname: Jiang
authors.affiliation: School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055, China. lizg@pkusz.edu.cn.
authors.forename: Kuan
authors.initials: K
authors.lastname: Hu
authors.affiliation: School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055, China. lizg@pkusz.edu.cn.
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Shi
authors.affiliation: Department of Chemistry, The Chinese University of Hong Kong, Shatin, Hong Kong SAR, China.
authors.forename: Qingzhuang
authors.initials: Q
authors.lastname: Tang
authors.affiliation: Shenzhen Middle School, Shenzhen 518001, China.
authors.forename: ZiChen
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Department of Gynecology, Shenzhen People's Hospital, Shenzhen 518055, China.
authors.forename: Xiyang
authors.initials: X
authors.lastname: Ye
authors.affiliation: School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055, China. lizg@pkusz.edu.cn.
authors.forename: Zigang
authors.initials: Z
authors.lastname: Li
mesh_terms: D001665:Binding Sites; D047628:Estrogen Receptor alpha / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D008958:Models, Molecular; D010455:Peptides / Q000737:chemistry*
chemical_list: C506487:ESR1 protein, human; D047628:Estrogen Receptor alpha; D010455:Peptides