Lysine-specific demethylase 5A (KDM5A, also named RBP2 or JARID1A) is a demethylase that can remove methyl groups from histones H3K4me1/2/3. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, drug resistance, and is associated with poor prognosis. Pharmacological inhibition of KDM5A has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of KDM5A, its role in carcinogenesis, a comparison of currently available approaches for screening KDM5A inhibitors, a classification of KDM5A inhibitors, and its potential as a drug target in cancer therapy.

赖氨酸特异性去甲基化酶 5A（KDM5A，也称为 RBP2 或 JARID1A）是一种去甲基化酶，可以去除组蛋白 H3K4me1/2/3 中的甲基。它在许多癌症中异常表达，阻碍分化并导致癌细胞增殖、细胞转移和侵袭性、耐药性，并与预后不良有关。据报道，KDM5A 的药理学抑制可显着减弱一系列实体瘤和急性髓细胞白血病的体外和体内肿瘤进展。这篇综述将介绍 KDM5A 的结构方面、其在致癌作用中的作用、目前可用的 KDM5A 抑制剂筛选方法的比较、KDM5A 抑制剂的分类及其作为癌症治疗药物靶点的潜力。