NR2F6 Modulators Reprogram Immune Cells to Reduce Tumors

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Solution Overview

Problem

Current methods for treating diseases, particularly cancer, face challenges in effectively modulating the immune system to target cancer cells, as immune checkpoints like CTLA-4 and PD-1 are prematurely activated, allowing tumors to evade immune attack, and existing therapies lack specificity in targeting NR2F6 activity.

Innovation Solution

Development of novel compounds that modulate NR2F6 activity, acting as agonists or antagonists to reprogram immune cells, specifically activating or inhibiting NR2F6 targets in isolated immune cells to enhance immune responses against tumors, and administering these compounds to patients to treat autoimmune disorders and cancer.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing therapies target immune checkpoints like CTLA-4 and PD-1, then immune responses against tumors can be enhanced, but immune checkpoints are prematurely activated allowing tumors to evade immune attack

Engineering Contradiction:
Improveimmune response effectivenessVSAvoidtumor evasion capability
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by blocking immune checkpoint activation before tumors can exploit them for evasion. The compounds prevent the premature activation of CTLA-4 and PD-1 pathways, ensuring immune cells remain functional and ready to attack tumor cells before the tumor can establish immune evasion mechanisms.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses small molecule compounds as intermediaries to modulate immune checkpoint activity. These compounds act as mediators between the immune system and tumor cells, specifically targeting NR2F6 to regulate immune checkpoint expression and function, thereby enhancing immune response while preventing tumor evasion.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Measurement precision

If small molecules are designed to directly inhibit oncogenic proteins, then genotype-selective anti-tumor activity can be achieved, but specificity in targeting NR2F6 activity is lacking in existing therapies

Engineering Contradiction:
Improvetargeting specificityVSAvoidtherapy customization
Core Design Contradiction:
Measurement precisionVSAdaptability or versatility

Solution Approach 1:

The patent applies local quality by designing compounds with specific structural features that target NR2F6 activity in particular cellular contexts. The compounds exhibit selective modulation of NR2F6-dependent gene expression in immune cells versus other cell types, achieving local specificity in their biological effect while maintaining the ability to address different cancer genotypes.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses parameter changes by modifying molecular structure parameters of the small compounds to optimize their binding affinity and selectivity for NR2F6. By adjusting parameters such as molecular weight, functional groups, and stereochemistry, the compounds achieve high specificity for NR2F6 while maintaining versatility in treating different cancer types with NR2F6 involvement.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS10472351B2Small molecule agonists and antagonists of NR2F6 activity in animals
Publication Date: 2019.11.12 SYBLEU INC
  • US10472351B2 patent drawing
  • US10472351B2 patent drawing
  • US10472351B2 patent drawing

AI summary

The present technology is directed to modulators of nuclear receptor activity, specifically to the modulation of NR2F6 activity and NR2F6 utilizing compounds, and the immune modulation and modulation of cancer stem cell activity through administration of compounds described herein to animals.