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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Targeting mTOR for fighting diseases: A revisited review of mTOR inhibitors
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Targeting mTOR for fighting diseases: A revisited review of mTOR inhibitors

机译：针对战斗疾病的MTOR：重新审查MTOR抑制剂

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摘要

mTOR (mammalian target of rapamycin), which is a serine/threonine kinase, has been well-established as being closely correlated with the occurrence of various human diseases, such as tumors and neurodegenerative diseases. Inhibition of the mTOR signaling pathways may effectively block the abnormal signal transduction of various growth factors and thereby block the occurrence and development of diseases. Of note, first-generation mTOR inhibitors are mainly reported to be rapamycin and its derivatives and second-generation mTOR inhibitors that consist of several ATP-competitive kinase inhibitors. Interestingly, the third-generation mTOR inhibitor, RapaLink-1, mediates rapamycin and mTOR kinase inhibitors via the same molecule and shows much higher efficiency. In addition, there are many mTOR inhibitors that have potential therapeutic effects for tumors and other types of diseases. Thus, we focus on summarizing the basic structures of mTOR and its complexes, some key upstream and downstream signaling pathways, and the structures and characteristics of the three generations of mTOR inhibitors in disease. Together, these findings may provide a better understanding of mTOR-regulated mechanisms and their inhibitors for fighting human diseases in the near future. (C) 2020 Elsevier Masson SAS. All rights reserved.
机译：MTOR（哺乳动物的雷帕霉素靶标）是丝氨酸/苏氨酸激酶，已经很好地确定与各种人类疾病的发生密切相关，例如肿瘤和神经变性疾病。 MTOR信号传导途径的抑制可以有效地阻断各种生长因子的异常信号转导，从而阻止疾病的发生和发展。值得注意的是，第一代MTOR抑制剂主要据报道是雷帕霉素及其衍生物和第二代MTOR抑制剂，其由几种ATP竞争激酶抑制剂组成。有趣的是，第三代MTOR抑制剂Rapalink-1，通过相同的分子介导雷帕霉素和MTOR激酶抑制剂，效率更高。此外，有许多MTOR抑制剂对肿瘤和其他类型的疾病具有潜在的治疗效果。因此，我们专注于总结MTOR及其复合物的基本结构，一些关键上游和下游信号通路，以及三代疾病的三代MTOR抑制剂的结构和特征。这些发现可以在一起可以更好地了解MTOR调节机制及其在不久的将来对抗人类疾病的抑制剂。 （c）2020 Elsevier Masson SAS。版权所有。

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