Department of Chemical and Biomolecular Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon, Republic of Korea.
Department of Bioengineering, College of Engineering, Hanyang University, Seoul, Republic of Korea.
J Control Release. 2017 Oct 28;264:24-33. doi: 10.1016/j.jconrel.2017.08.001. Epub 2017 Aug 1.
Artificial cationic helical peptides possess an enhanced cell-penetrating property. However, their cell-penetrability is not converted by cellular environmental changes resulting in nonspecific uptake. In this study, pH-sensitive anion-donating groups were added to a helical polypeptide to simultaneously achieve tumor targeting and pro-apoptotic activity. The mitochondria-destabilizing helical polypeptide undergoing pH-dependent conformational transitions selectively targeted cancer cells consequently disrupting mitochondrial membranes and subsequently inducing apoptosis. This work presents a promising peptide therapeutic system for cancer therapy.
人工阳离子螺旋肽具有增强的细胞穿透性。然而，它们的细胞穿透性不会因细胞环境变化而转化，导致非特异性摄取。在这项研究中，将 pH 敏感的阴离子供体基团添加到螺旋多肽中，以同时实现肿瘤靶向和促凋亡活性。经历 pH 依赖性构象转变的线粒体破坏螺旋多肽选择性靶向癌细胞，从而破坏线粒体膜并随后诱导细胞凋亡。这项工作为癌症治疗提供了一种很有前途的肽治疗系统。
