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Identification of osimertinib (AZD9291) as a lysine specific demethylase 1 inhibitor.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2018-11-16 , DOI: 10.1016/j.bioorg.2018.11.018
Zhong-Rui Li 1 , Feng-Zhi Suo 1 , Bo Hu 1 , Yan-Jia Guo 1 , Dong-Jun Fu 1 , Bin Yu 2 , Yi-Chao Zheng 1 , Hong-Min Liu 1
Affiliation  

Osimertinib (AZD9291) is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that has been approved for the treatment of EGFR-mutated non-small cell lung cancer (NSCLC). In this study, osimertinib was characterized as a LSD1 inhibitor for the first time with an IC50 of 3.98 ± 0.3 μM and showed LSD1 inhibitory effect at cellular level. These findings provide new molecular skeleton for dual inhibitor for LSD1 and EGFR. Osimertinib could serve as a lead compound for further development for anti-NSCLC drug discovery with dual targeting.

中文翻译:

确定奥西替尼(AZD9291)为赖氨酸特异性脱甲基酶1抑制剂。

Osimertinib(AZD9291)是第三代表皮生长因子受体(EGFR)酪氨酸激酶抑制剂(TKI),已被批准用于治疗EGFR突变的非小细胞肺癌(NSCLC)。在这项研究中,osimertinib首次被表征为LSD1抑制剂,IC50为3.98±0.3μM,并在细胞水平上显示出LSD1抑制作用。这些发现为LSD1和EGFR的双重抑制剂提供了新的分子骨架。Osimertinib可以作为双靶向靶向抗NSCLC药物发现的进一步开发的先导化合物。
更新日期:2018-11-16
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