The role of PRMT1 in cellular regulation and disease: Insights into biochemical functions and emerging inhibitors for cancer therapy

IF 4.3 3区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutical Sciences Pub Date : 2024-11-07 DOI:10.1016/j.ejps.2024.106958

Shiyao Ma , Shanhui Yi , Hui Zou , Shasha Fan , Yin Xiao

引用次数: 0

Abstract

Protein Arginine Methyltransferase 1 (PRMT1), a primary protein arginine methyltransferase, plays a pivotal role in cellular regulation, influencing processes such as gene expression, signal transduction, and cell differentiation. Dysregulation of PRMT1 has been linked to the development of various cancers, establishing it as a key target for therapeutic intervention. This review synthesizes the biochemical characteristics, structural domains, and functional mechanisms of PRMT1, focusing on its involvement in tumorigenesis. Additionally, the development and efficacy of emerging PRMT1 inhibitors as potential cancer therapies are examined. By employing molecular modeling and insights from existing literature, this review posits that targeting PRMT1’s methyltransferase activity could disrupt cancer progression, providing valuable insights for future drug development.

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PRMT1 在细胞调控和疾病中的作用：洞察生化功能和用于癌症治疗的新兴抑制剂。

蛋白精氨酸甲基转移酶 1（PRMT1）是一种初级蛋白精氨酸甲基转移酶，在细胞调控中发挥着关键作用，影响着基因表达、信号转导和细胞分化等过程。PRMT1 的失调与各种癌症的发生有关，因此成为治疗干预的关键靶点。本综述综述了 PRMT1 的生化特征、结构域和功能机制，重点介绍了它在肿瘤发生中的参与。此外，还研究了作为潜在癌症疗法的新兴 PRMT1 抑制剂的开发和疗效。通过利用分子建模和现有文献中的见解，本综述认为针对 PRMT1 的甲基转移酶活性可以破坏癌症的进展，为未来的药物开发提供有价值的见解。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

European Journal of Pharmaceutical Sciences 医学-药学

CiteScore

9.60

自引率

2.20%

发文量

248

审稿时长

50 days

期刊介绍： The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.