There is growing evidence for a causal role of the KDM5 family of histone demethylases in human cancer. In particular, KDM5A (JARID1A/RBP2) and KDM5B (JARID1B/PLU1) contribute to cancer cell proliferation, reduce the expression of tumor suppressor genes, promote the development of drug tolerance and …

Lysine-specific demethylase 5A is an enzyme that in humans is encoded by the KDM5A gene. [5][6] The protein encoded by this gene is a ubiquitously expressed nuclear protein. It binds directly, with several other proteins, to retinoblastoma protein which regulates cell proliferation. It was formerly known as Retinoblastoma Binding Protein 2 (RBP2).

KDM5）是JMJD（jumonji domain containing）家族 中重要的一员，通过特异性去除组蛋白 3第4位赖 氨酸（H3K4）甲基化修饰，参与表观遗传调控过 程，与肿瘤、免疫、耐药等疾病的发生发展有密切 关系[6-8]。作为一个潜在的肿瘤治疗靶标，KDM5的

kdm5b是一种组蛋白去甲基化酶，是kdm5 4种亚型中的一种，参与表观遗传调控过程，与肿瘤等疾病有密切关系。上述结果表明kdm5b可能是icb响应低的生物标志物，靶向kdm5b可能诱导t细胞浸润并克服对icb的耐药性，这引起了研究人员极大的兴趣。

Aug 5, 2021 · KDM5 inhibition reverts the effects of KMT2D mutations by increasing levels of H3K4me3 and restoring expression of KMT2D-regulated genes. Loss-of-function mutations in KMT2D are a striking feature of germinal center (GC) lymphomas, resulting in decreased histone 3 lysine 4 (H3K4) methylation and altered gene expression.

Dec 12, 2022 · In this review, we adopt a unique perspective regarding the context-dependent roles of KDM5A and KDM5B in development and tumorigenesis. It is well known that these two proteins show a high degree...

kdm5抑制剂对干扰素信号通路的激活作用，可以显著提高细胞对病毒感染的抵抗力。 随后，研究人员用 CRISPR/Cas9技术 ，逐个敲除涉及干扰素信号通路激活的基因，并检测其对KDM5抑制剂作用的影响。

Oct 20, 2021 · Here we show that, in mouse melanoma models, depletion of KDM5B—an H3K4 demethylase that is critical for melanoma maintenance and drug resistance 13, 14, 15 —induces robust adaptive immune...

Here, we provide an overview of the roles of KDM5 in cancer, explore the molecular mechanisms through which KDM5 regulates transcriptional output, including our recent finding that KDM5A supports transcriptional activation by controlling the H3K4 methylation cycle, and further discuss the possibility of the use of KDM5 inhibitors in cancer therapy.

May 20, 2024 · Several KDM5 inhibitors have shown potent BC inhibitory activity in vitro and in vivo, but challenges still exist in developing KDM5 inhibitors. In this review, we introduce the subtypes of BC and their current therapeutic options, summarize KDM5 family context-specific functions in the pathobiology of BC, and discuss the outlook and pitfalls ...