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Updated: Jun 12, 2026
10:51
Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Farnesoid X receptor modulators: a patent review
1Origin Pharmaceuticals, Inc., Wayne, PA 19087, USA. mlcrawley@originpharmaceuticals.com
Expert Opinion on Therapeutic Patents
|June 24, 2010
Summary
New farnesoid X receptor (FXR) agonists show promise for treating dyslipidemia. These compounds are effective and safe in preclinical studies, offering potential new therapies for cholesterol management and other conditions.
Area of Science:
- Pharmacology
- Biochemistry
- Drug Discovery
Background:
- Farnesoid X receptor (FXR) regulates cholesterol, triglyceride, and lipogenesis pathways.
- Dyslipidemia treatment requires novel medications due to statin intolerance.
- FXR agonists represent a promising therapeutic avenue for metabolic disorders.
Purpose of the Study:
- To review recent advances in novel FXR modulators.
- To focus on patent applications and publications from the last five years.
Main Methods:
- Systematic review of 72 patent applications and peer-reviewed articles.
- Analysis of 16 generic structure classes and nearly 5000 synthesized structures.
- Survey of structure-activity relationships, in vitro, and in vivo efficacy.
Main Results:
- Identified 16 distinct structural classes of FXR modulators.
- Nearly 5000 novel compounds were synthesized and analyzed.
- Revealed insights into structure-activity relationships and therapeutic potential.
Conclusions:
- FXR agonists demonstrate efficacy and safety in primate models.
- Significant potential exists for treating dyslipidemia.
- Potential applications extend to other disease areas beyond metabolic disorders.
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