UDP-Sugar Therapy for PGM1-CDG Glycosylation Restoration

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Solution Overview

Problem

There is no proven effective treatment available for most types of congenital disorders of glycosylation (CDGs), which are caused by defects in glycoprotein and glycolipid synthesis, leading to severe phenotypes and symptoms such as cardiomyopathies, endocrinopathies, and coagulopathy.

Innovation Solution

Administering a composition including UDP-galactose and UDP-glucose to patients with CDGs, particularly those with phosphoglucomutase 1 deficiency (PGM1-CDG), to restore depleted levels of these sugars and restart stalled glycosylation processes, thereby reducing symptom severity and improving glycosylation status.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If no treatment is administered to CDG patients, then the disease progresses with severe phenotypes and symptoms, but administering conventional treatments does not effectively restore glycosylation

Engineering Contradiction:
Improvetreatment effectivenessVSAvoiddisease severity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses UDP-galactose and UDP-glucose as intermediary substances to bridge the metabolic defect in PGM1-CDG. These nucleotide sugars act as direct substrates that bypass the defective phosphoglucomutase enzyme, allowing glycosylation pathways to proceed despite the enzymatic blockage. This intermediary approach directly addresses the metabolic bottleneck without requiring correction of the underlying genetic defect.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The treatment involves changing the concentration parameters of specific metabolites (UDP-galactose and UDP-glucose) in the patient's system. By administering these sugars at therapeutic doses, the patent alters the metabolic parameter landscape to overcome the enzymatic deficiency. The specific dosage regimen aims to achieve sufficient intracellular concentrations to restore glycosylation flux despite the enzyme defect.

Inventive Principle:
Principle #35Parameter changes

2Manufacturing precision

If UDP-galactose and UDP-glucose are administered to restore glycosylation, then glycosylation status improves and symptom severity reduces, but the complexity of treatment protocol increases

Engineering Contradiction:
Improveglycosylation restorationVSAvoidtreatment protocol complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent employs a dual-substrate treatment approach where UDP-galactose and UDP-glucose work synergistically to address multiple aspects of the glycosylation defect. These two nucleotide sugars serve multiple functions: they directly supplement depleted substrates, maintain proper UDP-sugar pool ratios, and potentially activate alternative metabolic pathways. This multi-functionality allows a single treatment regimen to address various manifestations of the disease.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The treatment protocol involves preliminary administration of UDP-galactose and UDP-glucose to establish adequate substrate pools before glycosylation can be restored. This preliminary supplementation ensures that when glycosylation pathways become active, sufficient substrates are available to prevent accumulation of intermediate metabolites and enable proper protein glycosylation from the outset.

Inventive Principle:
Principle #10Preliminary action

3Productivity

If oral galactose is administered to restore UDP-galactose levels, then glycosylation restarts in PGM1-CDG patients, but the metabolic pathway complexity increases

Engineering Contradiction:
Improveglycosylation rateVSAvoidmetabolic pathway complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent segments the glycosylation restoration process into distinct metabolic steps: oral galactose absorption, conversion to UDP-galactose via Leloir pathway enzymes, and subsequent utilization in glycosylation reactions. By understanding and targeting specific segments of this pathway (particularly the UDP-galactose generation step), the treatment can optimize galactose supplementation to overcome the PGM1 defect without requiring complete pathway reconstruction.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP3806866B1Methods and materials for treating glycosylation disorders
Publication Date: 2022.11.16 MAYO FOUNDATION FOR MEDICAL EDUCATION & RESEARCH
  • EP3806866B1 patent drawingFigure 1
  • EP3806866B1 patent drawingFigure 2
  • EP3806866B1 patent drawingFigure 3A~3C

AI summary

This document provides methods and materials involved in treating congenital disorders of glycosylation (CDGs). For example, methods for using a composition including one or more uridine diphosphate (UDP) - sugars to treat a mammal (e.g., a human) having a CDG are provided.