DCG066(DCG066) - 药物靶点：EHMT2_在研适应症：白血病_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

EHMT2

作用机制

EHMT2抑制剂(euchromatic histone lysine methyltransferase 2 inhibitors)

治疗领域

肿瘤血液及淋巴系统疾病

在研适应症

白血病

非在研适应症-

原研机构

Georgia State University

在研机构

Georgia State University

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C30H31F6N3O2

InChIKeyPMPKMTDYPOAEEH-UHFFFAOYSA-N

CAS号494786-13-9

关联

100 项与 DCG066 相关的临床结果

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100 项与 DCG066 相关的转化医学

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100 项与 DCG066 相关的专利（医药）

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1

项与 DCG066 相关的文献（医药）

2024-07-01·Annals of Hematology

Novel methyltransferase G9a inhibitor induces ferroptosis in multiple myeloma through Nrf2/HO-1 pathway

Article

作者: Zang, Lanlan ; Wang, Xiaoshun ; Xue, Renyu ; Li, Xiaoqi ; Zhang, Yu ; Xiong, Xingfang ; Wang, Zhiqiang ; Wang, Lijuan

Multiple myeloma (MM) is a common malignant hematologic neoplasm, and the involvement of epigenetic modifications in its development and drug resistance has received widespread attention. Ferroptosis, a new ferroptosis-dependent programmed death mode, is closely associated with the development of MM. The novel methyltransferase inhibitor DCG066 has higher cell activity, but its mechanism of action in MM has not been clarified. Here, we found that DCG066 (5µM) inhibited the proliferation and induced ferroptosis in MM cells; the intracellular levels of ROS, iron, and MDA were significantly elevated, and the level of GSH was reduced after the treatment of DCG066; The protein expression levels of SLC7A11, GPX4, Nrf2 and HO-1 were significantly reduced, and these phenomena could be reversed by ferroptosis inhibitor Ferrostatin-1 (Fer-1) and Nrf2 activator Tert-butyl hydroquinone (TBHQ). Meanwhile, the protein expression levels of Keap1 was increased, and heat shock proteins (HSP70, HSP90 and HSPB1) were reduced after DCG066 treatment. In conclusion, this study confirmed that DCG066 inhibits MM proliferation and induces ferroptosis via the Nrf2/HO-1 pathway.

100 项与 DCG066 相关的药物交易

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