Li group published article on Angew Chem Int Ed about a study of crosslinked aspartic acids as helix-nucleating templates
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.
This article was published in the “Angewandte Chemie” (Hui Zhao‡ , Qi-Song Liu‡ , Hao Geng‡ , Yuan Tian, Min Cheng, Yan-Hong Jiang, MingSheng Xie, Xiao-Gang Niu, Fan Jiang, Ya-Ou Zhang, Yuan-Zhi Lao, Yun-Dong Wu,* NaiHan Xu,* and Zi-Gang Li* “Crosslinked Aspartic Acids as Helix-Nucleating Templates” Angew. Chem.Int. Ed.2016 DOI: 10.1002/ange.201606833)
Linking: http://onlinelibrary.wiley.com/doi/10.1002/ange.201606833/pdf