靶向 FXR 调节剂以实现肠道特异性：最新进展和研究进展。
Tailoring FXR Modulators for Intestinal Specificity: Recent Progress and Insights.
机构信息
Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, MO 63110, USA.
Department of Anesthesiology, Washington University School of Medicine in St. Louis, St. Louis, MO 63110, USA.
出版信息
Molecules. 2024 Apr 27;29(9):2022. doi: 10.3390/molecules29092022.
While FXR has shown promise in regulating bile acid synthesis and maintaining glucose and lipid homeostasis, undesired side effects have been observed in clinical trials. To address this issue, the development of intestinally restricted FXR modulators has gained attention as a new avenue for drug design with the potential for safer systematic effects. Our review examines all currently known intestinally restricted FXR ligands and provides insights into the steps taken to enhance intestinal selectivity.
尽管 FXR 在调节胆汁酸合成和维持葡萄糖及脂质内稳态方面显示出良好的前景，但在临床试验中观察到了一些不理想的副作用。为了解决这个问题，开发肠道限制性 FXR 调节剂作为一种新的药物设计途径引起了人们的关注，这种途径可能具有更安全的系统性作用。我们的综述检查了所有目前已知的肠道限制性 FXR 配体，并深入探讨了增强肠道选择性所采取的步骤。
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