State Key laboratory of Chemical Oncogenomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055, P. R. China.
Chem Commun (Camb). 2019 Apr 4;55(29):4198-4201. doi: 10.1039/c9cc01027k.
Peptides that induced autophagy at micromolar concentrations with improved proteolytic resistance properties were generated using the facile methionine bis-alkylation method. Notably, a short bicyclic peptide 7f was proven to be the most potent one among the designed peptides in regards to autophagy inducing activity. This study facilitated the development of a peptide-based autophagy inducer and demonstrated the potential applications of the methionine alkylation-based macrocyclization method for the diversity-oriented generation of peptide-based autophagy inducers.
使用简便的蛋氨酸双烷基化方法生成了在微摩尔浓度下诱导自噬且具有改善的蛋白水解抗性的肽。值得注意的是，在所设计的肽中，短双环肽 7f 在诱导自噬活性方面被证明是最有效的。这项研究促进了基于肽的自噬诱导剂的开发，并展示了基于蛋氨酸烷基化的大环化方法在多样性导向的基于肽的自噬诱导剂生成方面的应用潜力。
