Modulation of Conformational Transition of Polypeptides under Slightly Acidic Environment?

作者：Li, Jie; Zhang, Jiajie; Long, Qi; Guo, Weisheng; Xiong, Menghua^*

来源：Chinese Journal of Chemistry, 2022, 40(24): 2981-2987.

DOI：10.1002/cjoc.202200483

• Peptides
• Conformational transition
• Helical structures
• pH responsiveness
• Drug delivery

Comprehensive Summary Controlling the conformational transition of polypeptides under slightly acidic environment is challenging. Herein, we report a class of pH-responsive helix-to-coil conformationally transitionable polypeptides (pCTPs) by simply conjugating tertiary amine groups (TAs) to polylysine. Their conformation is highly dependent on the charge state of TAs, showing a helical structure when most TAs are deprotonated and a non-helical structure when majority of TAs are protonated. The conformational transition pH can be modulated by tuning the hydrophobicity of TAs and the incorporation of hydrophobic monomers at a pH range of 7.2 to 6.0. Such pCTP showed a vesicle-to-micelle transition when their conformation transformed from helix to coil, facilitating controlled drug release. Our study provided an approach to control the conformational transition of polypeptides under slightly acidic condition.

• 单位
  广州医学院; 1