mTOR kinase inhibitors as potential cancer therapeutic drugs.
mTOR kinase inhibitors as potential cancer therapeutic drugs.
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DOI：
10.1016/j.canlet.2013.06.017
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发表时间：
2013-10-28
期刊：
影响因子：
9.7
通讯作者：
Sun, Shi-Yong
中科院分区：
文献类型：
--
作者：
Sun, Shi-Yong
哺乳动物rapamycin靶点（mTOR）主要通过与raptor（形成mTORC复合物1；mTORC1）或rictor（形成mTOR复合物2；mTORC2）的直接相互作用，在细胞生长和存活的正向调节中发挥关键作用。mTOR轴在许多类型的癌症中经常被激活，因此已成为一个有吸引力的癌症治疗靶点。传统的mTOR变抑抑制剂雷帕霉素及其类似物（rapalogs）优先抑制mTORC1，在大多数类型的癌症中具有适度的临床抗癌活性，这促使人们努力开发既抑制mTORC1又抑制mTORC2的mTOR激酶抑制剂（TORKinibs），以期开发出比rapalogs具有更好治疗效果的新一代mTOR抑制剂。已经开发了几种torkinib，并积极进行临床前和临床研究。本文将重点介绍TORKinibs开发和研究的最新进展，并讨论该领域的一些潜在问题或挑战。
The mammalian target of rapamycin (mTOR) plays a critical role in the positive regulation of cell growth and survival primarily through direct interaction with raptor (forming mTORC complex 1; mTORC1) or rictor (forming mTOR complex 2; mTORC2). The mTOR axis is often activated in many types of cancer and thus has become an attractive cancer therapeutic target. The modest clinical anticancer activity of conventional mTOR allosteric inhibitors, rapamycin and its analogues (rapalogs), which preferentially inhibit mTORC1, in most types of cancer, has encouraged great efforts to develop mTOR kinase inhibitors (TORKinibs) that inhibit both mTORC1 and mTORC2, in the hope of developing a novel generation of mTOR inhibitors with better therapeutic efficacy than rapalogs. Several TORKinibs have been developed and actively studied preclinically and clinically. This review will highlight recent advances in the development and research of TORKinibs and discuss some potential issues or challenges in this area.
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影响因子：
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DOI：
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发表时间：
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期刊：
Clinical cancer research : an official journal of the American Association for Cancer Research
影响因子：
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