Rac1 in human diseases: The therapeutic potential of targeting Rac1 signaling regulatory mechanisms.
Rac1 in human diseases: The therapeutic potential of targeting Rac1 signaling regulatory mechanisms.
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DOI：
10.1080/21541248.2016.1211398
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发表时间：
2017-07-03
期刊：
影响因子：
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通讯作者：
Malliri A
中科院分区：
文献类型：
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作者：
Marei H;Malliri A
Rac1信号异常与许多使人衰弱的疾病有关，包括癌症、心血管疾病和神经退行性疾病。因此，Rac1代表了一个有吸引力的治疗靶点，但有效的Rac1抑制剂的研究仍在进行中。考虑到与Rac1信号扰动相关的不利影响，细胞已经进化出几种机制来确保Rac1信号的严格调节。因此，表征这些机制可以提供有关导致Rac1信号异常的主要细胞事件的宝贵信息。重要的是，这些信息可用于进一步促进可恢复正常Rac 1信号传导的有效药理调节剂的开发。在这篇综述中，我们专注于Rac1信号的病理作用，突出了在临床环境中靶向Rac1的好处和潜在的缺点。此外，我们提供了一个可用的化合物，目标的关键Rac1调节机制的概述，并讨论了未来的治疗途径，从我们对这些机制的理解。
Abnormal Rac1 signaling is linked to a number of debilitating human diseases, including cancer, cardiovascular diseases and neurodegenerative disorders. As such, Rac1 represents an attractive therapeutic target, yet the search for effective Rac1 inhibitors is still underway. Given the adverse effects associated with Rac1 signaling perturbation, cells have evolved several mechanisms to ensure the tight regulation of Rac1 signaling. Thus, characterizing these mechanisms can provide invaluable information regarding major cellular events that lead to aberrant Rac1 signaling. Importantly, this information can be utilized to further facilitate the development of effective pharmacological modulators that can restore normal Rac1 signaling. In this review, we focus on the pathological role of Rac1 signaling, highlighting the benefits and potential drawbacks of targeting Rac1 in a clinical setting. Additionally, we provide an overview of available compounds that target key Rac1 regulatory mechanisms and discuss future therapeutic avenues arising from our understanding of these mechanisms.