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Cellular, Structural Basis, and Recent Progress for Targeting Murine Double Minute X (MDMX) in Tumors
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-08-26 , DOI: 10.1021/acs.jmedchem.4c00913
Qikun Yin 1 , Yuemiao Hu 1 , Zhiwen Dong 1 , Jing Lu 1 , Hongbo Wang 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-08-26 , DOI: 10.1021/acs.jmedchem.4c00913
Qikun Yin 1 , Yuemiao Hu 1 , Zhiwen Dong 1 , Jing Lu 1 , Hongbo Wang 1
Affiliation
Murine double minute X (MDMX) is an oncoprotein that mainly has a negative regulatory effect on the tumor suppressor p53 to induce tumorigenesis. As MDMX is highly expressed in various types of tumor cells, targeting and inhibiting MDMX are becoming a promising strategy for treating cancers. However, the high degree of structural homology between MDMX and its homologous protein murine double minute 2 (MDM2) is a great challenge for the development of MDMX-targeted therapies. This review introduces the structure, distribution, and regulation of the MDMX, summarizes the structural features and structure–activity relationships (SARs) of MDMX ligands, and focuses on the differences between MDMX and MDM2 in these aspects. Our purpose of this work is to propose potential strategies to achieve the specific targeting of MDMX.
中文翻译:
靶向小鼠双分钟 X (MDMX) 肿瘤的细胞、结构基础和最新进展
鼠双分钟X(MDMX)是一种癌蛋白,主要对抑癌基因p53产生负调节作用,从而诱导肿瘤发生。由于 MDMX 在各种类型的肿瘤细胞中高表达,靶向和抑制 MDMX 正在成为治疗癌症的一种有前景的策略。然而,MDMX与其同源蛋白鼠双分钟2(MDM2)之间的高度结构同源性对于MDMX靶向治疗的开发是一个巨大的挑战。本文介绍了MDMX的结构、分布和调控,总结了MDMX配体的结构特征和构效关系(SAR),并重点讨论了MDMX与MDM2在这些方面的差异。我们这项工作的目的是提出潜在的策略来实现 MDMX 的特定目标。
更新日期:2024-08-26
中文翻译:
靶向小鼠双分钟 X (MDMX) 肿瘤的细胞、结构基础和最新进展
鼠双分钟X(MDMX)是一种癌蛋白,主要对抑癌基因p53产生负调节作用,从而诱导肿瘤发生。由于 MDMX 在各种类型的肿瘤细胞中高表达,靶向和抑制 MDMX 正在成为治疗癌症的一种有前景的策略。然而,MDMX与其同源蛋白鼠双分钟2(MDM2)之间的高度结构同源性对于MDMX靶向治疗的开发是一个巨大的挑战。本文介绍了MDMX的结构、分布和调控,总结了MDMX配体的结构特征和构效关系(SAR),并重点讨论了MDMX与MDM2在这些方面的差异。我们这项工作的目的是提出潜在的策略来实现 MDMX 的特定目标。