Promoter-Driven DREADD Compositions for Retina-to-Locus Coeruleus Targeting

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Solution Overview

Problem

Current therapeutic treatments for diseases and disorders of the nervous system lack cell-type specificity, leading to inefficacy and neurosurgical complications when targeting brain regions like the locus coeruleus.

Innovation Solution

Utilizing promoter-driven Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) expressed in retinal cells, specifically through the use of adeno-associated viral vectors, to stimulate targeted neurological pathways, particularly the locus coeruleus, via natural circuit inputs, avoiding direct brain injection.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If direct brain injection of DREADDs is used to target locus coeruleus, then cell-type specificity is improved, but neurosurgical risks and complexity increase

Engineering Contradiction:
Improvecell-type specificityVSAvoidneurosurgical risks
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent uses the retina as an intermediary structure to deliver DREADDs indirectly to the locus coeruleus. By injecting DREADDs into the retina (a more accessible and safer location), the compounds naturally traffic through retinal ganglion cell axons to reach the locus coeruleus in the brain, avoiding direct brain surgery while achieving cell-type specificity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent segments the delivery process into two distinct stages: first, delivery of DREADDs to the retina via safe intravitreal or subretinal injection; second, natural transport through retinal ganglion cell axons to the locus coeruleus. This segmentation allows the complex brain delivery task to be broken into safer, manageable steps.

Inventive Principle:
Principle #1Segmentation

2Reliability

If direct brain injection of DREADDs is used to target locus coeruleus, then treatment efficacy is improved, but procedural complexity increases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidprocedural complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent employs the retinal ganglion cell axon pathway as a natural intermediary transport system. This biological highway automatically carries DREADDs from the retina to the locus coeruleus, eliminating the need for complex stereotactic brain injection procedures while maintaining reliable delivery to the target nucleus.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent leverages the body's own neural pathways to perform the delivery function. Retinal ganglion cells naturally project to the locus coeruleus, and this endogenous transport mechanism is harnessed to deliver DREADDs without requiring external surgical intervention in the brain, effectively making the biological system serve the delivery function.

Inventive Principle:
Principle #25Self-service

3Adaptability or versatility

If non-specific therapeutic treatments are used for nervous system diseases, then treatment scope is improved, but cell-type specificity deteriorates

Engineering Contradiction:
Improvetreatment scopeVSAvoidcell-type specificity
Core Design Contradiction:
Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent applies local quality by making the DREADD expression location-specific through retinal targeting. The promoter-driven expression system ensures DREADDs are selectively expressed in retinal ganglion cells, and consequently in the locus coeruleus, providing localized modulation of this specific nucleus while leaving other brain regions unaffected.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent changes the spatial parameter of DREADD expression from diffuse brain injection to focused retinal delivery. This parameter change results in concentrated, specific expression in the locus coeruleus via natural axonal transport, transforming a non-specific treatment approach into a precisely targeted therapy.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3507371B1Compositions for treating diseases and disorders of the nervous system
Publication Date: 2026.01.28 RUTGERS THE STATE UNIV
  • EP3507371B1 patent drawingFigure 1
  • EP3507371B1 patent drawingFigure 2A~2D
  • EP3507371B1 patent drawingFigure 3A~3F

AI summary

Methods and compositions for treating diseases or disorders of the nervous system using promoter-driven Designer Receptor Exclusively Activated by Designer Drugs (DREADDs) and DREADD agonists are disclosed.