2-Deoxy-Monosaccharide Esters for Selective Glycolysis Inhibition

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current glycolytic inhibition approaches for cancer treatment are not specific to hypoxic tumor cell environments and can interfere with normal cell functions, such as glycosylation, leading to clinical consequences, and there is a need for improved methods to treat proliferative diseases like cancer and inflammatory dermatological conditions.

Innovation Solution

Administration of therapeutically effective amounts of 2-deoxy-monosacharide esters or their salts/prodrugs, specifically compounds of Formula I, which selectively target glycolytic pathways in tumor cells, thereby inhibiting glycolysis without affecting normal cellular energy production pathways.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current glycolytic inhibition treatments are used, then tumor cell growth is inhibited, but normal cell function is also affected due to lack of specificity

Engineering Contradiction:
Improveselectivity of glycolytic inhibitionVSAvoidinterference with normal cell glycosylation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing compounds that specifically target hypoxic environments where tumor cells reside. The 2-deoxy-monosaccharide esters are structurally modified to preferentially accumulate in hypoxic regions and selectively inhibit glycolysis in these localized areas, while leaving normal aerobic cells unaffected. This resolves the contradiction by making the inhibition spatially selective rather than system-wide.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by modifying the chemical structure of traditional glycolytic inhibitors into 2-deoxy-monosaccharide ester derivatives with specific physicochemical properties. These structural modifications alter the compounds' selectivity parameters, enabling them to distinguish between hypoxic tumor cells and normoxic normal cells, thereby inhibiting glycolysis selectively in tumor cells without affecting normal cell glycosylation pathways.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If glycolysis is inhibited in tumor cells, then tumor cell death is achieved, but normal cells that rely on glycolysis may also be harmed

Engineering Contradiction:
Improveanti-proliferative efficacyVSAvoiddamage to normal cells
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses hypoxia-inducible factors and specific transport mechanisms as intermediaries to deliver the 2-deoxy-monosaccharide esters preferentially to hypoxic tumor cells. These intermediaries act as selective carriers that recognize and transport the compounds into hypoxic environments, ensuring that glycolytic inhibition is mediated specifically in tumor cells while normal aerobic cells remain protected.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent segments the cellular metabolism pathways by designing compounds that specifically interfere with the glycolytic pathway in hypoxic conditions while leaving other energy production pathways intact. The 2-deoxy-monosaccharide esters are structurally segmented to target only the glycolytic enzyme machinery in hypoxic cells, allowing normal cells to maintain their glycolysis and use alternative pathways without harm.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS11925654B2Esters of 2-deoxy-monosaccharides with anti proliferative activity
Publication Date: 2024.03.12 BOARD OF RGT THE UNIV OF TEXAS SYST
  • US11925654B2 patent drawing
  • US11925654B2 patent drawing
  • US11925654B2 patent drawing

AI summary

Compounds and methods of using the same to inhibit glycolysis and treat cancer and other diseases are disclosed.