Key Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, People's Republic of China.
Methods Mol Biol. 2022;2530:169-175. doi: 10.1007/978-1-0716-2489-0_12.
Stapled peptides have received widespread attention in therapeutics due to the superior membrane penetration and in vivo stability. We have developed a series of methods including CIH, TD coupling, Met-Met, and Cys-Met bis-alkylation strategy to switch peptides' secondary structure and enhance their stability and cellular uptake. Here we focus on the peptide macrocyclization method of Met-Met and Cys-Met bis-alkylation strategy to generate more stable and permeable sulfonium-tethered peptides to avoid tedious synthesis, which can be utilized for drug delivery and further broad biological applications.
由于具有优越的膜穿透性和体内稳定性，订书肽在治疗学中受到了广泛关注。我们开发了一系列方法，包括 CIH、TD 偶联、Met-Met 和 Cys-Met 双烷基化策略，以改变肽的二级结构，提高其稳定性和细胞摄取能力。在这里，我们重点介绍 Met-Met 和 Cys-Met 双烷基化策略的肽大环化方法，以生成更稳定和可渗透的锍键肽，避免繁琐的合成，可用于药物输送和进一步广泛的生物学应用。
