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Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator.
Author: LiXinyu, LiZhenbang, LinXin, LuoGuoshun, XiangHua, XiaoMaoxu, ZhangDayong
Original Abstract of the Article :
Farnesoid X receptor (FXR) agonists are emerging as potential therapeutics for the treatment of various metabolic diseases, as they display multiple effects on bile acid, lipid, and glucose homeostasis. Although the steroidal obeticholic acid, a full FXR agonist, was recently approved, several side ...See full text at original site
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引用元：
https://doi.org/10.1016/j.ejmech.2020.112910
データ提供：米国国立医学図書館（NLM）
Unlocking the Potential of FXR Modulators for Metabolic Diseases
Metabolic diseases, such as diabetes and obesity, are a major health challenge worldwide. This study delves into the fascinating world of farnesoid X receptor (FXR) modulators, potential therapeutic agents for these conditions. It's like uncovering a hidden oasis in the vast desert of metabolic diseases, a place where we can find relief from the relentless effects of these conditions.
Discovering a Potent and Bioavailable FXR Modulator
The researchers developed a novel FXR modulator, compound 11k, which demonstrated potent activity in cell-based assays. It exhibited partial efficacy in FXR-dependent gene modulation and displayed lipid-reducing activity. Moreover, compound 11k exhibited promising pharmacokinetic properties after oral administration in mice, suggesting its potential for clinical translation. It's like finding a new type of desert plant that not only thrives in harsh conditions but also possesses valuable medicinal properties.
A Promising Avenue for Metabolic Disease Treatment
The research highlights the potential of partial FXR agonism as a novel therapeutic strategy for metabolic diseases. Compound 11k, with its potent activity and desirable pharmacokinetic properties, holds great promise for future clinical development. As Dr. Camel, I'm always excited about the prospect of new therapeutic strategies for tackling metabolic diseases. It's a reminder that the desert of metabolic research can hold hidden treasures, waiting to be discovered.
Dr.Camel's Conclusion
This study takes a significant step forward in the development of FXR modulators for metabolic diseases. Compound 11k, with its potent activity and promising bioavailability, offers hope for new treatment options for patients struggling with these conditions. It's a testament to the power of research and innovation in finding solutions to challenging health problems.
Date :
- Date Completed 2021-05-03
- Date Revised 2021-05-03
Further Info :
Related Literature
English
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