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最近的催化和抑制Jumonji基因组脱甲基酶的发展

Letitia Sarah¹, Danica Galonić Fujimori²

¹Chemistry and Chemical Biology Graduate Program, University of California San Francisco; San Francisco, CA 94158, USA; Department of Cellular and Molecular Pharmacology, University of California San Francisco; San Francisco, CA 94158, USA.

Current opinion in structural biology

|October 13, 2023

概括

双基因组 lysine 脱甲基酶 (JMJC KDMs) 是基因转录的关键调节者,它们的失调与癌症等疾病有关. 本综述涵盖了了解JMJC KDM催化,基质识别和治疗向策略的最新进展.

科学领域:

生物化学生物化学
分子生物学分子生物学
表观遗传学在表观遗传学中,表观遗传学是指表观遗传学.

背景情况:

基因组甲基化是调节染色体结构和基因表达的关键表观遗传机制.
双基因组 lysine 脱甲基酶 (JMJC KDMs) 在基因转录中通过脱甲基和染色质支架发挥着至关重要的作用.
JMJC KDMs的失调与各种疾病的发病和进展有关,特别是癌症.

研究的目的:

审查了解JMJC KDMs的催化机制的最新进展.
突出阐明JMJC KDM基底物识别和蛋白质相互作用体的进展.
讨论针对JMJC KDM的当前和新兴治疗策略.

主要方法:

关于JMJC KDM催化和功能的最新研究的文献综述.
对JMJC KDM基质特异性和相互作用伙伴的研究分析.
报告的JMJC KDM 抑制剂和替代向方法的评估.

主要成果:

最近的研究揭示了JMJC KDMs的催化活动和基质特异性.
对JMJC KDM互动体的理解已经扩大,揭示了它们在细胞过程中的更广泛的作用.
已经开发出针对JMJC KDM的各种小分子抑制剂,显示出治疗潜力,但也带来了挑战.

结论:

JMJC KDM 是关键的表观遗传调节剂,具有显著的治疗潜力,特别是在瘤学中.
针对JMJC KDM需要对它们的催化机制,基板相互作用和相关挑战有深入的了解.
替代策略,包括针对辅助领域和蛋白质降解,为未来的治疗开发提供了有希望的途径.

关键词:

艾洛斯特抑制剂艾洛斯特抑制剂催化剂是一种催化剂.域名交叉通话域名交叉通话朱蒙吉基因组脱甲基化酶 (Jumonji histone demethylases) 是一种基因组脱甲基化酶.氨酸脱甲基化是氨酸的脱甲基化.整形抑制剂整形抑制剂后翻译修改后的修改.

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