Vitamin D Assay Using FRET and Modified VDR-LBD

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current methods for measuring vitamin D derivatives, such as 25-hydroxyvitamin D, are not sufficiently sensitive or specific, particularly in patients with chronic kidney disease or bone disorders, where accurate monitoring is crucial to prevent adverse effects on calcium and phosphorus metabolism.

Innovation Solution

A method using a modified ligand-binding domain of the vitamin D receptor (VDR) with enhanced affinity for 25-hydroxyvitamin D, combined with Fluorescence Resonance Energy Transfer (FRET) technology, allows for precise measurement of vitamin D derivatives by detecting conformational changes induced by ligand binding, utilizing donor-acceptor fluorophores like SCFP3A and SYFP2.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If current methods for measuring vitamin D derivatives are used, then the measurement process is simple, but the sensitivity and specificity are insufficient

Engineering Contradiction:
Improvesensitivity and specificity of vitamin D measurementVSAvoidcomplexity of measurement method
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent introduces a modified VDR-LBD protein as an intermediary component that specifically binds to vitamin D derivatives. This modified protein contains fluorophores that undergo FRET (Fluorescence Resonance Energy Transfer) when the vitamin D derivative binds, providing a sensitive and specific detection mechanism. The intermediary protein serves as a bridge between the vitamin D molecule and the detection system, enabling precise measurement while maintaining manageable complexity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces conventional mechanical or chemical measurement approaches with a fluorescence-based optical detection system. By using fluorophores attached to the modified VDR-LBD that emit light signals upon vitamin D binding, the system achieves high sensitivity and specificity through optical detection rather than traditional measurement methods.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Measurement precision

If conventional measurement assays are used, then the assay procedure is straightforward, but the ability to detect conformational changes and measure vitamin D levels accurately is limited

Engineering Contradiction:
Improveaccuracy of vitamin D derivative concentration detectionVSAvoiddifficulty of detecting conformational changes
Core Design Contradiction:
Measurement precisionVSDifficulty of detecting and measuring

Solution Approach 1:

The patent utilizes fluorescence intensity changes as a detectable signal when vitamin D derivatives bind to the modified VDR-LBD. The fluorophores attached to the protein undergo changes in their fluorescent properties (analogous to color changes) upon ligand binding, providing a clear and measurable signal that indicates both the occurrence of binding and the conformational changes in the protein structure.

Inventive Principle:
Principle #32Color changes

Solution Approach 2:

The patent replaces direct measurement of conformational changes with fluorescence signal detection. Instead of attempting to directly measure the physical conformational changes in the protein, the system uses fluorophores that report these changes through changes in their optical properties, making the detection process more sensitive and easier to measure.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Measurement precision

If high affinity binding is achieved through modified VDR-LBD, then the specificity for 25-hydroxyvitamin D increases, but the complexity of the receptor structure increases

Engineering Contradiction:
Improvespecificity for 25-hydroxyvitamin DVSAvoidcomplexity of modified VDR-LBD structure
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent applies local quality by making specific, targeted modifications to the VDR-LBD structure rather than completely redesigning the entire receptor. The modifications are localized to specific regions of the protein that are critical for vitamin D binding, such as introducing fluorophores at strategic positions or making point mutations that enhance affinity for 25-hydroxyvitamin D while preserving the overall protein structure and function.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The modified VDR-LBD can be viewed as a composite structure combining the natural vitamin D receptor protein with synthetic fluorophore molecules. This composite approach allows the protein to retain its natural binding specificity while the attached fluorophores provide the detection capability, achieving both high specificity and detectability without requiring complete redesign of the receptor.

Inventive Principle:
Principle #40Composite materials

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

This approach provides a rapid, clinically accessible, and highly sensitive assay for measuring vitamin D levels, enabling accurate detection of 25-hydroxyvitamin D concentrations, thereby aiding in the diagnosis and management of vitamin D deficiency and related disorders.

Implementation Method 1

Fluorescence Resonance Energy Transfer (FRET) and a modified ligand-binding domain of the vitamin D receptor (LBD-VDR) to measure vitamin D derivatives

Methodology Applied
Scientific EffectFluorescence Resonance Energy Transfer (FRET):

Implementation Method 2

detecting conformational changes induced by ligand binding

Methodology Applied
Scientific EffectConformational change:

Data Source

PatentEP2427484B1Method and composition for measuring the amount of vitamin d derivatives
Publication Date: 2016.07.06 OPKO IRELAND GLOBAL HOLDINGS LTD(GB)
  • EP2427484B1 patent drawingFigure 1A
  • EP2427484B1 patent drawingFigure 1B
  • EP2427484B1 patent drawingFigure 2

AI summary

Methods and compositions for measuring the amount of vitamin D derivatives are disclosed. Fluorescence Resonance Energy Transfer (FRET) in combination with a modified ligand-binding domain of the vitamin D receptor (LBD-VDR) to measure vitamin D derivatives are also disclosed.