LRH-1 Modulator Compounds for Therapeutic Applications

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Solution Overview

Problem

Current endogenous phospholipid ligands for Liver Receptor Homolog-1 (LRH-1) are not optimal for probing LRH-1 biology or serving as drug leads, given its critical roles in various diseases such as inflammatory bowel disease, liver and cardiovascular diseases, and cancers.

Innovation Solution

Development of specific compounds that act as LRH-1 agonists, with diverse structural variations including bonds, alkylene, and electrophilic moieties, which can modulate LRH-1 activity for therapeutic applications, including pharmaceutical compositions and methods for treating associated diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If endogenous phospholipid ligands are used for LRH-1, then the receptor can be activated, but they are not optimal for probing LRH-1 biology or serving as drug leads

Engineering Contradiction:
Improveefficacy as drug leadsVSAvoidsuitability for probing biology
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent modifies the chemical structure of phospholipid ligands by changing parameters such as the head group, fatty acid chains, and molecular weight to create synthetic analogs that maintain LRH-1 binding affinity while improving pharmacological properties for therapeutic applications

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining elements of natural phospholipids with synthetic modifications, resulting in hybrid ligands that exhibit both high receptor specificity and improved drug-like properties for therapeutic use

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS10980755B2LRH-1 modulators
Publication Date: 2021.04.20 RGT UNIV OF CALIFORNIA
  • US10980755B2 patent drawing
  • US10980755B2 patent drawing
  • US10980755B2 patent drawing

AI summary

Disclosed herein are compositions and methods for modulating the liver receptor homolog-1.