查尔酮
法尼甾体X受体
敌手
细胞生长
癌症研究
药理学
转移
对抗
化学
抑制性突触后电位
受体
生物
内科学
癌症
医学
核受体
生物化学
立体化学
转录因子
基因
作者
Sheng Niu,Guoning Zhang,Na Wang,Guangyao Lv,Jinsong Liu,Hongbo Wang,Wei‐Shuo Fang
出处
期刊:ChemMedChem
[Wiley]
日期:2022-03-11
卷期号:17 (11)
被引量:1
标识
DOI:10.1002/cmdc.202100778
摘要
Abstract Although the farnesoid X receptor (FXR) has been regarded as a promising drug target for metabolic diseases as well as anti‐inflammatory, antitumor and antiviral actions, the antagonism by FXR ligands are still underrepresented in current FXR targeted therapies. In this study, we discovered selective FXR antagonists through structure optimization from the polyoxygenated chalcone scaffold. The selective antagonist 6 p [2‐methoxy‐2’‐hydroxy‐4’‐(4’’‐methoxy‐4’’‐oxo‐ E ‐crotonyl) chalcone] is not only inhibitory toward non‐small‐cell lung cancer (NSCLC) cell proliferation in an FXR‐dependent manner, but is also active in metastasis models. Taken together, this chalcone‐based FXR antagonist has the potential for the targeted therapy of NSCLC in which FXR is highly expressed.
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