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首页> 外文期刊>Current opinion in gastroenterology >Farnesoid X receptor agonists in biliary tract disease.
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Farnesoid X receptor agonists in biliary tract disease.

机译：法尼醇X受体激动剂可治疗胆道疾病。

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摘要

The farnesoid X receptor (FXR) is a member of ligand-activated nuclear receptor superfamily. FXR is a bile sensor and is part of a complex network of nuclear receptors that includes also the constitutive androstane receptor and the pregnane X receptor. These receptors act coordinately to regulate essential steps of bile acids and xenobiotics uptake, metabolism and excretion in hepatocytes, cholangiocytes and kidney cells. Preclinical models indicate that FXR agonists are effective in reducing liver injury in nonobstructive models of cholestasis. FXR ligands are currently under investigation for treating patients with early stage primary biliary cirrhosis. Although these ligands hold promise, evidence is growing that FXR activation could impair the expression/activity of basolateral transporters such as multidrug resistance protein 4 essential for basolateral secretion of bile constituents in the systemic circulation. Because FXR, pregnane X receptor and constitutive androstane receptor ligands interact with different target genes, it appear that a combination with pregnane X receptor, constitutive androstane receptor ligand/activator or both or ursodeoxycholic acid could prevent possible side-effects of FXR activation in severe cholestasis.
机译：法尼醇X受体（FXR）是配体激活的核受体超家族的成员。 FXR是一个胆汁传感器，是复杂的核受体网络的一部分，该网络还包括组成型雄烷烃受体和孕烷X受体。这些受体协同作用以调节肝细胞，胆管细胞和肾细胞中胆汁酸和异种生物的摄取，代谢和排泄的基本步骤。临床前模型表明，在非阻塞性胆汁淤积模型中，FXR激动剂可有效减少肝损伤。 FXR配体目前正在研究中，以治疗早期原发性胆汁性肝硬化患者。尽管这些配体有希望，但越来越多的证据表明，FXR激活可能会损害基底外侧转运蛋白的表达/活性，例如对于全身循环中胆汁成分的基底外侧分泌必不可少的多药耐药蛋白4。由于FXR，孕烷X受体和组成型雄烷受体配体与不同的靶基因相互作用，因此看来，与孕烷X受体，组成性雄烷受体配体/激活剂或两者结合或熊去氧胆酸可以预防FXR激活在严重胆汁淤积中的副作用。

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