title: Crosslinked Aspartic Acids as Helix-Nucleating Templates.
abstract: Described is a facile helix-nucleating template based on a tethered aspartic acid at the N-terminus [terminal aspartic acid (TD)]. The nucleating effect of the template is subtly influenced by the substituent at the end of the side-chain-end tether as indicated by circular dichroism, nuclear magnetic resonance, and molecular dynamics simulations. Unlike most nucleating strategies, the N-terminal amine is preserved, thus enabling further modification. Peptidomimetic estrogen receptor modulators (PERMs) constructed using this strategy show improved therapeutic properties. The current strategy can be regarded as a good complement to existing helix-stabilizing methods.
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China.
authors: Hui
authors: H
authors: Zhao
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China.|Shenzhen Key Lab of Tissue Engineering, The Second People's Hospital of Shenzhen, Shenzhen, 518035, China.
authors: Qi-Song
authors: QS
authors: Liu
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China.
authors: Hao
authors: H
authors: Geng
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China.
authors: Yuan
authors: Y
authors: Tian
authors: Key Lab in Healthy Science and Technology, Division of Life Science, Shenzhen Graduate School of Tsinghua University, Shenzhen, 518055, China.
authors: Min
authors: M
authors: Cheng
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China.
authors: Yan-Hong
authors: YH
authors: Jiang
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China.
authors: Ming-Sheng
authors: MS
authors: Xie
authors: College of Chemistry and Molecular Engineering, Beijing Nuclear Magnetic Resonance Center, Peking University, Beijing, 100871, China.
authors: Xiao-Gang
authors: XG
authors: Niu
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China.
authors: Fan
authors: F
authors: Jiang
authors: Key Lab in Healthy Science and Technology, Division of Life Science, Shenzhen Graduate School of Tsinghua University, Shenzhen, 518055, China.
authors: Ya-Ou
authors: YO
authors: Zhang
authors: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.
authors: Yuan-Zhi
authors: YZ
authors: Lao
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China. wuyd@pkusz.edu.cn.
authors: Yun-Dong
authors: YD
authors: Wu
authors: Key Lab in Healthy Science and Technology, Division of Life Science, Shenzhen Graduate School of Tsinghua University, Shenzhen, 518055, China. xu.naihan@sz.tsinghua.edu.cn.
authors: Nai-Han
authors: NH
authors: Xu
authors: School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, 518055, China. lizg@pkusz.edu.cn.
authors: Zi-Gang
authors: ZG
authors: Li
keywords: amino acids; circular dichroism; helical structures; peptides; protein-protein interactions