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Discovery of novel ketoxime ether derivatives with potent FXR agonistic activity, oral effectiveness and high liver/blood ratio.

Author: GuYipei, LengYing, NingMengmeng, ShenJianhua, TangXuehang, YanHongyi, YeYangliang

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

This study reports the development of novel non-steroidal farnesoid X receptor (FXR) agonists that show potent FXR agonistic activities in vitro and effectively promote target gene expression in vivo. The compounds have a high liver/blood ratio, potentially reducing side effects associated with systemic FXR activation.
Paper Details　
Original Abstract of the Article :
The farnesoid X receptor (FXR) is a promising therapeutic target for nonalcoholic steatohepatitis (NASH) and other bile acid related diseases because it plays a critical role in fibrosis, inflammation and bile acid homeostasis. Obeticholic acid (OCA), a FXR agonist which was synthesized from chenode...See full text at original site
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引用元：
https://doi.org/10.1016/j.bmc.2021.116280

データ提供：米国国立医学図書館（NLM）

Discovery of novel ketoxime ether derivatives with potent FXR agonistic activity

This research delves into the exciting realm of drug discovery for nonalcoholic steatohepatitis (NASH), a liver disease that has become increasingly prevalent. It's like searching for a hidden oasis in the desert of liver disease research, hoping to find a cure. The authors focus on the Farnesoid X Receptor (FXR), a crucial target for developing new NASH treatments. They have discovered a promising new class of FXR agonists, compounds 13j and 13z, which not only show potent activity in the lab but also demonstrate good bioavailability, meaning they are well absorbed by the body. This research represents a significant advancement in the development of effective and safe NASH treatments.

Promising new avenues for treatment

This study offers a glimmer of hope in the fight against NASH. The discovery of these novel FXR agonists represents a potential breakthrough in treating this debilitating disease. It's like finding a spring of fresh water in the heart of the desert, providing a source of relief and healing.

A healthy liver, a healthy life

NASH is a serious condition, and this research offers hope for those affected. By continuing to invest in research and development, we can one day find a cure for NASH, allowing everyone to enjoy a healthy liver and a healthy life.

Dr. Camel's Conclusion

This research is a testament to the power of scientific innovation. Like a tenacious camel caravan crossing a harsh desert, scientists are tirelessly searching for solutions to challenging medical problems. This discovery offers a promising new path forward in the fight against NASH.
Date :
  1. Date Completed 2021-12-29
  2. Date Revised 2021-12-29
Further Info :

Pubmed ID

34256254

DOI: Digital Object Identifier

10.1016/j.bmc.2021.116280

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Article Analysis
・Side Effects of obeticholic acid
SNS
PICO Info
in preparation
Languages

English

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