非经典 MEK 抑制剂：MEK3-7 抑制剂的综述。
Non-'classical' MEKs: A review of MEK3-7 inhibitors.
机构信息
Department of Chemistry, Center for Molecular Innovation and Drug Discovery, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208, United States.
Department of Chemistry, Center for Molecular Innovation and Drug Discovery, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208, United States.
出版信息
Bioorg Med Chem Lett. 2020 Jul 1;30(13):127203. doi: 10.1016/j.bmcl.2020.127203. Epub 2020 Apr 23.
Abstract
The MAPK pathways are an enduring area of interest due to their essential roles in cell processes. Increased expression and activity can lead to a multitude of diseases, sparking research efforts in developing inhibitors against these kinases. Though great strides have been made in developing MEK1/2 inhibitors, there is a notable lack of chemical probes for MEK3-7, given their central role in stimuli response, cell growth, and development. This review summarizes the progress that has been made on developing small molecule probes for MEK3-7, the specific disease states in which they have been studied, and their potential to become novel therapeutics.
摘要
MAPK 通路因其在细胞过程中的重要作用而一直是研究的热点。表达和活性的增加可导致多种疾病，从而激发了针对这些激酶的抑制剂的研究工作。尽管在开发 MEK1/2 抑制剂方面已经取得了很大的进展，但鉴于 MEK3-7 在刺激反应、细胞生长和发育中的核心作用，针对它们的化学探针却明显缺乏。本文综述了用于 MEK3-7 的小分子探针的开发进展、它们在哪些特定疾病状态下得到了研究，以及它们作为新型治疗药物的潜力。
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