2021年6月3日 · Recently, two studies published in Nature identified genetic changes in the nuclear receptor-binding SET domain protein (NSD) family of histone methyltransferases as oncogenic drivers in some...

NSD3是一种组蛋白H3第36位赖氨酸 (H3K36)甲基转移酶，催化H3K36二甲基化，即增加两个甲基基团。 在2021年2月3日发表在Nature上的一篇论文中，Gozani教授及其合作者利用小鼠模型和人类肿瘤样本，将NSD3基因定义为肺鳞状细胞癌的致癌基因，也就说，NSD3的突变导致了失控的细胞增殖。 研究发现，在人类肿瘤中，NSD3变得失调，要么拷贝数增加，要么发生错义突变使其催化活性增加（错义突变指编码某种氨基酸的密码子经碱基替换以后,变成编码另一种氨基酸的 …

2024年2月3日 · NSD proteins recognize and catalyze methylation of histone lysine marks, thereby regulating chromatin integrity and gene expression. Multiple studies have implicated NSD proteins in human disease, noting impacts from translocations, aberrant expression, and various dysfunctional somatic mutations.

2024年4月1日 · The NSD family of H3K36 methyltransferase enzymes—including NSD1 (KMT3B), NSD2 (MMSET/WHSC1), and NSD3 (WHSC1L1)—are now receiving drug development attention, with the exciting advent of an NSD2 inhibitor (KTX-1001) advancing to Phase I clinical trials for relapsed or refractory multiple myeloma.

2023年8月5日 · Recently, Sun et al. [61] designed a drug molecule based on the PROTAC strategy that demonstrated effective inhibitory activity against lung cancer cells and NSD3 degradation in vitro and in vivo, once again highlighting the potential of NSD3 as a therapeutic approach for lung cancer.

2023年8月8日 · As a key member of NSD family proteins, NSD2 plays an important role in the pathogenesis and progression of various diseases such as cancers, inflammations, and infectious diseases, serving as a promising drug target. Developing potent and specific NSD2 inhibitors may provide potential novel therapeutics.

2023年8月24日 · Nuclear receptor binding SET domain proteins (NSDs) catalyze the mono- or dimethylation of histone 3 lysine 36 (H3K36me1 and H3K36me2), using S -adenosyl-l-methionine (SAM) as a methyl donor. As a key member of the NSD family of proteins, NSD2 plays an important role in the pathogenesis and pr …

2021年12月5日 · nsd蛋白家族是一类组蛋白赖氨酸甲基转移酶，在多种癌症中均存在扩增、变异、易位或过度表达情况。 近年来，随着对NSD1、NSD2和NSD3结构和功能研究的深入，以及首个治疗滤泡性淋巴瘤和上皮样肉瘤的HKMTase抑制剂Tazemettostat的获美国FDA批准成功上市，NSD抑制剂的 ...

2021年10月28日 · Nuclear receptor-binding SET domain (NSD) proteins are a class of histone lysine methyltransferases (HKMTases) that are amplified, mutated, translocated, or overexpressed in various types of cancers. Several campaigns to develop NSD inhibitors for cancer treatment have begun following recent advance …

2023年8月14日 · 核受体结合 set 结构域蛋白 （nsd） 使用 s-腺苷-l-蛋氨酸 （sam） 作为甲基供体，催化组蛋白 3 赖氨酸 36 （h3k36me1 和 h3k36me2） 的单甲基化或二甲基化。nsd2 作为 nsd 蛋白家族的关键成员，在癌症、炎症和传染病等多种疾病的发病机制和发展中发挥重要作用，是一 …