Interdisciplinary Science and Engineering in Health Systems, Okayama University, Okayama, Japan.
Department of Applied Chemistry, Kindai University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan.
Bioorg Med Chem Lett. 2021 Mar 15;36:127811. doi: 10.1016/j.bmcl.2021.127811. Epub 2021 Jan 21.
Pro-apoptotic peptides may be promising agents for cancer therapy owing to their ability to induce apoptosis in cancer cells. TatBim, a fusion peptide of Tat cell-penetrating peptide (CPP) and the BH3 domain derived from Bim apoptosis-inducing protein, is a pro-apoptotic peptide. In this study, based on the TatBim sequence, we attempted to minimize the CPP-Bim peptide while retaining apoptosis-inducing activity. The CPP and Bim parts were systematically shortened, and the pro-apoptotic activities of the shortened peptides were examined. We obtained TatBim-N1C2 and R8Bim-N1C2 as minimized peptides with efficient apoptotic activity. These peptides may have potential applications in future biomedical studies, such as cancer therapeutics.
促凋亡肽由于能够诱导癌细胞凋亡，因此可能成为癌症治疗的有前途的药物。TatBim 是一种由 Tat 细胞穿透肽 (CPP) 和来自 Bim 凋亡诱导蛋白的 BH3 结构域融合而成的促凋亡肽，是一种促凋亡肽。在这项研究中，基于 TatBim 序列，我们试图在保留诱导凋亡活性的同时最小化 CPP-Bim 肽。CPP 和 Bim 部分被系统缩短，并检测缩短肽的促凋亡活性。我们得到了具有高效凋亡活性的最小肽 TatBim-N1C2 和 R8Bim-N1C2。这些肽在未来的生物医学研究中可能具有应用潜力，例如癌症治疗。
