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The conjugation of rhodamine B enables carrier-free mitochondrial delivery of functional proteins.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-07-29 , DOI: 10.1039/d0ob01305f
Jiayuan Shi 1 , Dan Zhao , Xiang Li , Feng Ding , Xuemei Tang , Nian Liu , Hua Huang , Changlin Liu
Affiliation  

The development of protein-based therapeutics faces many challenges, for example, carrier-dependence, safety concerns, endocytosis-dependence, and uncertain in vivo therapeutic outcomes. Small molecules are rarely used for intracellular organelle-targeting and disease tissue-specific carrier-independent delivery of therapeutic proteins. Here, we report that rhodamine B, after modification with proteins, is able to guide carrier-free delivery into mitochondria and tissue-dependent distributions of functional proteins through organic cation transporters (OCTs). The enrichment of the modified catalase in the cancer tissue efficiently suppresses xenograft human lung tumor in mice. This carrier-free delivery platform of proteins may emerge as a simple yet powerful approach for cancer treatment.

中文翻译:


罗丹明 B 的结合能够实现功能蛋白的无载体线粒体递送。



基于蛋白质的疗法的发展面临许多挑战,例如载体依赖性、安全性问题、内吞作用依赖性以及不确定的体内治疗结果。小分子很少用于细胞内细胞器靶向和疾病组织特异性、不依赖载体的治疗蛋白递送。在此,我们报道罗丹明 B 在经过蛋白质修饰后,能够引导无载体递送至线粒体,并通过有机阳离子转运蛋白 (OCT) 引导功能蛋白的组织依赖性分布。癌组织中修饰过氧化氢酶的富集有效抑制小鼠异种移植人肺肿瘤。这种无载体的蛋白质递送平台可能会成为一种简单而强大的癌症治疗方法。
更新日期:2020-09-16
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