Yasheng Pharmaceutical's new and potent EED inhibitor research results are published on JMC

ArticleMedicine Guanlan

On October 18th, Yasheng Pharmaceutical announced that Dr.

Prior to this, Yasheng Pharmaceutical has obtained the exclusive global rights and interests in the development of EEDi-5273, and the company is currently making every effort to advance the preparations for the application of the candidate drug for clinical trials

The article published by Wang Shaomeng’s team is titled "Finding that EEDi-5273 is a very effective oral EED inhibitor that can achieve complete and long-lasting tumor regression

As mentioned in the article, Polycomb inhibitory complex 2 (PRC2) is a multi-protein complex, its core subunits include histone methyltransferase 2 (EZH2), EED, ZESTE 12 homolog 1 inhibitor 2 (SUZ12) and so on

In 2017, AbbVie and Novartis researchers discovered EED's allosteric inhibitors A-395 and EED226, respectively

Previous preclinical and clinical research results show that EZH2/EED inhibitors have broad application prospects in a variety of tumor and non-tumor indications

Compared with A-395 and EED226, the compound EEDi-5273 disclosed in this study has higher binding efficiency with EED, and can effectively inhibit the growth of KARPAS422 cells carrying the Y641N EZH2 mutation

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Reference materials:

[1] The research results of the new and potent EED inhibitor EEDi-5273 (APG-5918) were listed in the top journal of pharmaceutical chemistry JMC, which is expected to achieve complete tumor regression by regulating epigenetics.