肽基精氨酸脱亚胺酶(PADs)在疾病中的 作用及其抑制剂的研究进展
The Role of Peptidylarginine Deiminases (PADs) in Diseases and Research Progress on Their Inhibitors
DOI: 10.12677/acm.2026.1652050, PDF,   
作者: 张敏杰, 赵 丽*:中国药科大学基础医学与临床药学学院,江苏 南京
关键词: 肽基精氨酸脱亚胺酶(PADs)自身免疫性疾病肿瘤抑制剂Peptidylarginine Deiminases (PADs) Autoimmune Disease Tumor Inhibitor
摘要: 蛋白质的翻译后修饰是调节细胞功能及其多样性的关键机制。肽基精氨酸脱亚胺酶(PADs)是一类催化精氨酸转化为瓜氨酸(即瓜氨酸化)的钙依赖性酶家族。近年来的研究表明,PADs活性的失调与多种人类疾病密切相关。本文总结了PADs各亚型的组织分布及其在类风湿性关节炎、系统性红斑狼疮等自身免疫性疾病中通过产生自身抗原破坏免疫稳态的机制,详细探讨了PADs在不同肿瘤类型中调节细胞增殖、转移、血管生成及化疗耐药的复杂功能,归纳了包括小分子化合物和天然产物在内的PADs抑制剂的研发历程,旨在深化对PADs家族的理解,为PADs的功能及其抑制剂的研究提供参考。
Abstract: Post-translational modifications of proteins are crucial for regulating cellular function and diversity. The peptidylarginine deiminases (PADs) family consists of calcium-dependent enzymes that catalyze the citrullination of arginine residues. Recent studies have shown that dysregulation of PADs activity is closely associated with the development of numerous human diseases. This review systematically reviews the tissue distribution of PADs isoforms and delves into their pathogenic mechanisms in autoimmune diseases, such as rheumatoid arthritis and systemic lupus erythematosus, primarily through the generation of citrullinated autoantigens and the disruption of immune tolerance. Concurrently, the paper elaborates on the complex functions of PADs in various cancer types, including the regulation of tumor cell proliferation, invasion, metastasis, angiogenesis, and the induction of chemotherapy resistance. Furthermore, this review summarizes the development history and strategies of small-molecule inhibitors and natural products targeting PADs. The aim is to advance the understanding of the PADs family and provide references for the study of PADs functions and their inhibitors.
文章引用:张敏杰, 赵丽. 肽基精氨酸脱亚胺酶(PADs)在疾病中的 作用及其抑制剂的研究进展[J]. 临床医学进展, 2026, 16(5): 2405-2415. https://doi.org/10.12677/acm.2026.1652050

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