PROTACs在制药方向上的应用

Kechao Zhou, Li Zhang, Yi Liu
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引用次数: 1

摘要

蛋白水解靶向嵌合体(Proteolysis targeting chimeras, PROTACs)技术是一种新的药物开发策略,可以通过选择性降解靶向蛋白来治疗疾病。PROTACs由两个分子组成,一个分子与目标蛋白结合,另一个分子与蛋白质降解酶结合,从而促进目标蛋白的降解。与传统药物的作用机制相比,PROTAC技术具有高选择性、可逆性、低剂量效应等优点。PROTAC技术已广泛应用于多个领域,特别是在癌症研究中。PROTACs可以靶向癌症相关蛋白降解,从而抑制肿瘤生长和转移。例如,靶向BCL-2和BRD4等蛋白的PROTACs已被广泛研究并应用于癌症治疗。此外,PROTAC技术还可应用于神经退行性疾病、免疫治疗、代谢性疾病、感染性疾病等多个领域。尽管PROTAC技术具有广阔的应用前景,但仍存在一些挑战,如如何提高PROTAC的稳定性和药代动力学,以及如何大规模制备PROTAC。因此,还需要进一步的研究和优化,进一步完善PROTAC技术,促进其在临床治疗中的应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Application of PROTACs in the Pharmaceutical Direction
Proteolysis targeting chimeras (PROTACs) technology is a novel drug development strategy that can treat diseases by selectively degrading targeted proteins. PROTACs consist of two molecules, one of which binds to the target protein while the other binds to the protein degradation enzyme, thus promoting the degradation of the target protein. Compared to the mechanism of action of traditional drugs, PROTAC technology has many advantages, such as high selectivity, reversibility, and low dosage effects. PROTAC technology has been widely applied in multiple fields, especially in cancer research. PROTACs can target cancer-related proteins for degradation, thereby inhibiting tumor growth and metastasis. For instance, PROTACs targeting proteins such as BCL-2 and BRD4 have been extensively researched and applied in cancer treatment. In addition, PROTAC technology can also be applied to multiple fields such as neurodegenerative diseases, immunotherapy, metabolic diseases, and infectious diseases. Although PROTAC technology has broad application prospects, there are still some challenges, such as how to improve the stability and pharmacokinetics of PROTACs, and how to prepare large-scale PROTACs. Therefore, further research and optimization are still needed to further improve PROTAC technology and promote its application in clinical treatment.
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