化学
等甾体
甲状腺
甲状腺激素受体
三碘甲状腺素
脂肪变性
体内
激素
非酒精性脂肪性肝炎
内分泌学
受体
内科学
兴奋剂
药理学
生物化学
立体化学
非酒精性脂肪肝
医学
脂肪肝
生物
生物技术
疾病
作者
Thorsten Kirschberg,Christopher T. Jones,Yinchuan Xu,Martijn Fenaux,Randall L. Halcomb,Yujin Wang,Kevin Klucher
标识
DOI:10.1016/j.bmcl.2020.127465
摘要
Use of the oxadiazolone acid isostere in triiodothyronine analogs yielded potent and selective agonists for the thyroid hormone receptor β. Selected examples showed good in-vivo efficacy in a rat hypercholesterolemic model. One compound was further profiled in a diet-induced mouse model of nonalcoholic steatohepatitis (NASH) and showed robust target engagement and significant histological improvements in both liver steatosis and fibrosis.
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