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PROTACs: great opportunities for academia and industry.
Signal Transduction and Targeted Therapy ( IF 40.8 ) Pub Date : 2019-12-24 , DOI: 10.1038/s41392-019-0101-6 Xiuyun Sun 1, 2 , Hongying Gao 1, 2 , Yiqing Yang 1, 2 , Ming He 1 , Yue Wu 1 , Yugang Song 1 , Yan Tong 1 , Yu Rao 1, 3
Signal Transduction and Targeted Therapy ( IF 40.8 ) Pub Date : 2019-12-24 , DOI: 10.1038/s41392-019-0101-6 Xiuyun Sun 1, 2 , Hongying Gao 1, 2 , Yiqing Yang 1, 2 , Ming He 1 , Yue Wu 1 , Yugang Song 1 , Yan Tong 1 , Yu Rao 1, 3
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Although many kinds of therapies are applied in the clinic, drug-resistance is a major and unavoidable problem. Another disturbing statistic is the limited number of drug targets, which are presently only 20-25% of all protein targets that are currently being studied. Moreover, the focus of current explorations of targets are their enzymatic functions, which ignores the functions from their scaffold moiety. As a promising and appealing technology, PROteolysis TArgeting Chimeras (PROTACs) have attracted great attention both from academia and industry for finding available approaches to solve the above problems. PROTACs regulate protein function by degrading target proteins instead of inhibiting them, providing more sensitivity to drug-resistant targets and a greater chance to affect the nonenzymatic functions. PROTACs have been proven to show better selectivity compared to classic inhibitors. PROTACs can be described as a chemical knockdown approach with rapidity and reversibility, which presents new and different biology compared to other gene editing tools by avoiding misinterpretations that arise from potential genetic compensation and/or spontaneous mutations. PRTOACs have been widely explored throughout the world and have outperformed not only in cancer diseases, but also in immune disorders, viral infections and neurodegenerative diseases. Although PROTACs present a very promising and powerful approach for crossing the hurdles of present drug discovery and tool development in biology, more efforts are needed to gain to get deeper insight into the efficacy and safety of PROTACs in the clinic. More target binders and more E3 ligases applicable for developing PROTACs are waiting for exploration.
中文翻译：
PROTAC：学术界和工业界的巨大机遇。
尽管临床上应用了多种治疗方法，但耐药性是一个不可回避的主要问题。另一个令人不安的统计数据是药物靶点数量有限，目前仅占目前正在研究的所有蛋白质靶点的 20-25%。此外，目前对靶标的探索重点是它们的酶功能，而忽略了它们的支架部分的功能。作为一种有前途且有吸引力的技术，蛋白水解靶向嵌合体（PROTACs）因寻找解决上述问题的可行方法而引起了学术界和工业界的高度关注。PROTAC 通过降解而不是抑制靶蛋白来调节蛋白功能，从而提供对耐药靶点更高的敏感性以及影响非酶功能的更大机会。事实证明，与经典抑制剂相比，PROTAC 具有更好的选择性。PROTAC 可以被描述为一种快速且可逆的化学敲除方法，与其他基因编辑工具相比，它通过避免潜在的遗传补偿和/或自发突变引起的误解，呈现出新的和不同的生物学特性。PRTOAC 已在世界范围内得到广泛探索，不仅在癌症疾病方面表现出色，而且在免疫紊乱、病毒感染和神经退行性疾病方面也表现出色。尽管 PROTAC 提供了一种非常有前途且强大的方法来跨越目前生物学中药物发现和工具开发的障碍，但需要付出更多努力才能更深入地了解 PROTAC 在临床中的功效和安全性。更多适用于开发PROTAC的靶标结合物和E3连接酶正在等待探索。
更新日期：2019-12-24
中文翻译：
PROTAC：学术界和工业界的巨大机遇。
尽管临床上应用了多种治疗方法，但耐药性是一个不可回避的主要问题。另一个令人不安的统计数据是药物靶点数量有限，目前仅占目前正在研究的所有蛋白质靶点的 20-25%。此外，目前对靶标的探索重点是它们的酶功能，而忽略了它们的支架部分的功能。作为一种有前途且有吸引力的技术，蛋白水解靶向嵌合体（PROTACs）因寻找解决上述问题的可行方法而引起了学术界和工业界的高度关注。PROTAC 通过降解而不是抑制靶蛋白来调节蛋白功能，从而提供对耐药靶点更高的敏感性以及影响非酶功能的更大机会。事实证明，与经典抑制剂相比，PROTAC 具有更好的选择性。PROTAC 可以被描述为一种快速且可逆的化学敲除方法，与其他基因编辑工具相比，它通过避免潜在的遗传补偿和/或自发突变引起的误解，呈现出新的和不同的生物学特性。PRTOAC 已在世界范围内得到广泛探索，不仅在癌症疾病方面表现出色，而且在免疫紊乱、病毒感染和神经退行性疾病方面也表现出色。尽管 PROTAC 提供了一种非常有前途且强大的方法来跨越目前生物学中药物发现和工具开发的障碍，但需要付出更多努力才能更深入地了解 PROTAC 在临床中的功效和安全性。更多适用于开发PROTAC的靶标结合物和E3连接酶正在等待探索。
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