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Down‐regulating Proteolysis to Enhance Anticancer Activity of Peptide Nanofibers
Chemistry - An Asian Journal ( IF 3.5 ) Pub Date : 2018-07-24 , DOI: 10.1002/asia.201800875 Jie Li 1 , Xuewen Du 1 , Devon J Powell 1 , Rong Zhou 1 , Junfeng Shi 1 , Hongjian He 1 , Zhaoqianqi Feng 1 , Bing Xu 1
Chemistry - An Asian Journal ( IF 3.5 ) Pub Date : 2018-07-24 , DOI: 10.1002/asia.201800875 Jie Li 1 , Xuewen Du 1 , Devon J Powell 1 , Rong Zhou 1 , Junfeng Shi 1 , Hongjian He 1 , Zhaoqianqi Feng 1 , Bing Xu 1
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Nanofibers of short peptides are emerging as a promising type of agents for inhibiting cancer cells. But the proteolysis of peptides decreases the anticancer efficacy of the peptide nanofibers. Here we show that decreasing the activity of proteasomes enhance the activity of peptide nanofibers for inhibiting cancer cells. Based on the structure of galactin‐3, we designed a heptapeptide, which self‐assembles to form nanofibers. The nanofibers of the heptapeptide exhibit moderate cytotoxicity to three representative cancer cell lines (HeLa, MCF‐7, and HepG2), largely due to the proteolysis of the peptides. Using a clinically approved proteasome inhibitor, bortezomib, to treat the cancer cells significantly decreases the proteolysis of the peptides and enhances the activity of the peptide nanofibers for inhibiting the cancer cells. This work illustrates a promising approach for enhancing the anticancer efficacy of peptide nanofibers by modulating intracellular protein degradation machinery, as well as provides insights for understanding the cytotoxicity of aberrant protein or peptide aggregates in complicated cellular environment.
中文翻译：
下调蛋白水解增强肽纳米纤维的抗癌活性
短肽纳米纤维正在成为一种有前景的抑制癌细胞的药物。但肽的蛋白水解降低了肽纳米纤维的抗癌功效。在这里，我们发现降低蛋白酶体的活性可以增强肽纳米纤维抑制癌细胞的活性。基于galactin-3的结构，我们设计了一种七肽，它可以自组装形成纳米纤维。七肽的纳米纤维对三种代表性癌细胞系（HeLa、MCF-7 和 HepG2）表现出中等的细胞毒性，这主要是由于肽的蛋白水解作用。使用临床批准的蛋白酶体抑制剂硼替佐米治疗癌细胞，可显着降低肽的蛋白水解作用，并增强肽纳米纤维抑制癌细胞的活性。这项工作阐明了一种通过调节细胞内蛋白质降解机制来增强肽纳米纤维抗癌功效的有前途的方法，并为理解复杂细胞环境中异常蛋白质或肽聚集体的细胞毒性提供了见解。
更新日期：2018-07-24
中文翻译：
下调蛋白水解增强肽纳米纤维的抗癌活性
短肽纳米纤维正在成为一种有前景的抑制癌细胞的药物。但肽的蛋白水解降低了肽纳米纤维的抗癌功效。在这里，我们发现降低蛋白酶体的活性可以增强肽纳米纤维抑制癌细胞的活性。基于galactin-3的结构，我们设计了一种七肽，它可以自组装形成纳米纤维。七肽的纳米纤维对三种代表性癌细胞系（HeLa、MCF-7 和 HepG2）表现出中等的细胞毒性，这主要是由于肽的蛋白水解作用。使用临床批准的蛋白酶体抑制剂硼替佐米治疗癌细胞，可显着降低肽的蛋白水解作用，并增强肽纳米纤维抑制癌细胞的活性。这项工作阐明了一种通过调节细胞内蛋白质降解机制来增强肽纳米纤维抗癌功效的有前途的方法，并为理解复杂细胞环境中异常蛋白质或肽聚集体的细胞毒性提供了见解。
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