组蛋白甲基化是最常见的组蛋白修饰之一，也是基因转录调控的高动态调节因子。赖氨酸残基的甲基化可以改变染色质结构，有助于调节基于DNA的核活动。赖氨酸脱甲基化酶控制和维持影响染色质结构和细胞特性的表观遗传因子。多种疾病，包括恶性肿瘤，与它们的失调有关。生物化学和发病学的进展促进了小分子抑制剂和工具化合物的发现，这些化合物可以干扰赖氨酸脱甲基化。在本综述中，我们着重讨论JmjC域含有组蛋白赖氨酸脱甲基酶（KDM2-7）的结构和生物学作用、代表性抑制剂及其在癌症治疗中的治疗潜力，并旨在提供关于JmjC-KDM抑制剂的开发的独特见解。版权所有©2023 Elsevier Ltd。保留所有权利。

Histone methylation is the most common histone modification and a highly dynamic regulator of gene transcription. Methylation of lysine residues can alter the structure of chromatin, helping to regulate DNA-based nuclear activities. Lysine demethylases control and maintain epigenetic factors that affect chromatin structure and cell characteristics. A variety of diseases, including malignant tumors, are connected to their dysregulation. Advances in biochemistry and pathogenesis have prompted the discovery of small molecule inhibitors and tool compounds that disrupt lysine demethylation {AuQ: Edit OK?}. In this review, we focus on JmjC-domain-containing histone lysine demethylases (KDM2-7), discussing their structures and biological roles, representative inhibitors, and therapeutic potential in cancer therapy, and aiming to provide unique insights into the development of JmjC-KDM inhibitors.Copyright © 2023 Elsevier Ltd. All rights reserved.