Zou Le, Peng Qilin, Wang Ping, Zhou Boting
Department of Pharmacy, Xiangya Hospital, Central South University, No. 87, Xiangya Road, Changsha, 410008, Hunan Province, China.
Institute of Hospital Pharmacy, Central South University, Changsha, 410008, China.
J Membr Biol. 2017 Apr;250(2):115-122. doi: 10.1007/s00232-016-9940-z. Epub 2016 Dec 8.
Human immunodeficiency virus type I (HIV-1) transactivator of transcription (TAT) is encoded by HIV-1. It is a peptide rich in basic amino acids and belongs to the protein transduction domain family. It has been found that HIV-1 TAT and its core peptide segment TAT play an important role in promoting the cellular uptake of coupled bioactive macromolecules, such as peptides, proteins, oligonucleotides, and drug molecules. HIV-1 TAT can also significantly increase the soluble expression of extrinsic proteins. However, the mechanism behind the cellular uptake of HIV-1 TAT-derived cell-penetrating peptide remains unclear. This review focuses on the research into HIV-1 TAT-derived cell-penetrating peptide over the last years. We briefly discuss TAT's structural features, functions and applications, the mechanism of its cellular internalization, current challenges, and their possible solutions. At the end of this review, we provide a summary and predict the future research directions and potential applications of HIV-1 TAT when it is used as a cell-penetrating peptide.
人类免疫缺陷病毒I型（HIV-1）转录激活因子（TAT）由HIV-1编码。它是一种富含碱性氨基酸的肽，属于蛋白质转导结构域家族。研究发现，HIV-1 TAT及其核心肽段TAT在促进偶联的生物活性大分子（如肽、蛋白质、寡核苷酸和药物分子）的细胞摄取方面发挥着重要作用。HIV-1 TAT还能显著提高外源蛋白的可溶性表达。然而，HIV-1 TAT衍生的细胞穿透肽的细胞摄取背后的机制仍不清楚。本综述重点关注过去几年对HIV-1 TAT衍生的细胞穿透肽的研究。我们简要讨论了TAT的结构特征、功能和应用、其细胞内化机制、当前挑战及其可能的解决方案。在本综述结尾，我们进行了总结，并预测了HIV-1 TAT用作细胞穿透肽时的未来研究方向和潜在应用。
