首页|基于ERK1/2翻译后修饰调控及空间性调节的抗癌策略研究进展

基于ERK1/2翻译后修饰调控及空间性调节的抗癌策略研究进展

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ERK1/2是一种介导细胞信号转导的关键蛋白,参与调节细胞的染色质重塑、核解体、增殖、存活、代谢、迁移和分化等生物学过程.其过度激活与癌症的发生进展密切相关,机制表现为上游通路分子或调节因子的基因突变使ERK1/2过度激活及针对上述靶点进行抑制后的ERK1/2再激活.因而ERK1/2为一个有潜在价值的靶点.本文对ERK1/2的翻译后修饰调控及空间性调节的机制研究和相应小分子抑制剂的应用现状进行了讨论,总结并展望了目前靶向调控ERK1/2的抗癌策略及针对潜在靶点展开探索的可能性,为ERK1/2作为抗癌理想靶点的开发性研究提供了新思路.
Research Progress of Anti-cancer Strategies Based on ERK1/2 Post-translational Modification and Spatial Regulation
ERK1/2 is a key protein that mediates cell signal transduction,and it is involved in regulating biological processes such as chromatin remodeling,nuclear disintegration,proliferation,survival,metabolism,and cell migration and differentiation.Its overactivation is closely related to the occurrence and progression of cancer,and the mechanism is manifested as the overactivation of ERK1/2 by gene mutations of upstream pathway molecules or regulators and the reactivation of ERK1/2 after inhibition against the above targets.ERK1/2 is a potentially valuable target.In this review,the mechanism of post-translational modification and spatial regulation of ERK1/2 and the application status of corresponding small-molecule inhibitors were discussed.The current antitumor strategy of targeting and regulating ERK1/2 was summarized,and the possibility of exploring potential targets was elucidated,thus providing new insights into the developmental research of ERK1/2 as an ideal anticancer target.

ERK1/2TumorTargeted therapyPost-translational modificationsDimerizationSmall mole-cule inhibitor

虢婷、尚梦宇、郭茵、黄卫人

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530200 南宁,广西中医药大学研究生院

518061 深圳,深圳大学医学部基础医学院

515041 汕头,汕头大学医学院药理学教研室

518025 深圳,深圳市第二人民医院转化医学研究院

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ERK1/2 肿瘤 靶向治疗 翻译后修饰 二聚化 小分子抑制剂

国家重点研发计划国家自然科学基金青年科学基金深圳市科技创新项目

2019YFA090600082203459JCYJ20200109120016553

2024

肿瘤防治研究
湖北省卫生厅,中国抗癌协会,湖北省肿瘤医院

肿瘤防治研究

CSTPCD
影响因子:0.737
ISSN:1000-8578
年,卷(期):2024.51(6)