ERRβ Inverse Agonists for NAFLD Treatment
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Solution Overview
Problem
Current treatments for non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) lack effective solutions, particularly due to the lack of identified endogenous ligands for estrogen-related receptors (ERRs) which play a crucial role in metabolic regulation, including mitochondrial energetics and cholesterol metabolism.
Innovation Solution
Development of a method involving the administration of specific compounds, such as those with the provided chemical formulas, which act as selective inverse agonists for ERRβ, inhibiting its activity to treat NAFLD and NASH by modulating metabolic pathways.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for NAFLD and NASH are used, then existing therapeutic options are available, but effective solutions are lacking due to unmet clinical needs
Solution Approach 1:
The patent applies parameter changes by developing novel chemical compounds with specific molecular structures (Formula I) that can modulate ERRβ activity. By changing the chemical parameters and creating new ligand molecules, the invention provides effective treatments where previous options were lacking, directly addressing the contradiction between treatment effectiveness and availability of therapeutic options
Solution Approach 2:
The patent uses ERRβ modulators as intermediary substances that mediate between the administered compound and the metabolic pathways. These modulators act as intermediaries to regulate mitochondrial energetics, lipid metabolism, and glucose metabolism, thereby treating NAFLD and NASH when direct treatments were ineffective
2Reliability
If ERRβ activity is inhibited to treat metabolic disorders, then therapeutic benefit is achieved, but potential off-target effects on other nuclear receptors may occur
Solution Approach 1:
The patent applies local quality by designing compounds that selectively target ERRβ with specific binding characteristics. The molecular structure in Formula I is optimized to interact specifically with ERRβ's ligand-binding domain, ensuring that the therapeutic effect is localized to ERRβ modulation while minimizing interactions with other nuclear receptors, thus reducing off-target effects
Data Source
AI summary
Disclosed herein, inter alia, are compositions and methods useful for treating non-alcoholic fatty liver diseases.