Tu, Yalin; Sun, Yameng; Qiao, Shuang; Luo, Yao; Liu, Panpan; Jiang, Zhong-Xing; Hu, Yumin; Wang, Zifeng; Huang, Peng; Wen, Shijun published the artcile< Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma>, Product Details of C7H8BrN, the main research area is lymphoma EZH2 inhibitors degraders VHL CRBN YM181 YM281 antitumor.
Traditional EZH2 inhibitors are developed to suppress the enzymic methylation activity, and they may have therapeutic limitations due to the nonenzymic functions of EZH2 in cancer development. Here, we report proteolysis-target chimera (PROTAC)-based EZH2 degraders to target the whole EZH2 in lymphoma. Two series of EZH2 degraders were designed and synthesized to hijack E3 ligase systems containing either von Hippel-Lindau (VHL) or cereblon (CRBN), and some VHL-based compounds were able to mediate EZH2 degradation Two best degraders, YM181 (I) and YM281 (II), induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clin. used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degraders displayed promising antitumor activities in lymphoma xenografts and patient-derived primary lymphoma cells. Our study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Product Details of C7H8BrN.
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