Chimeric Protein Targeting TNF-Producing Cells

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Solution Overview

Problem

Current therapies for diseases involving excessive TNF activity, such as rheumatoid arthritis and cancer, often have limited efficacy as they primarily block TNF function rather than addressing the source of TNF production, leading to incomplete protection and potential side effects.

Innovation Solution

A chimeric protein comprising a cell-specific targeting agent, like the TNF binding protein, connected with Yersinia outer protein P (YopP) via a translocation polypeptide, allowing selective targeting and destruction of TNF-producing cells, thereby reducing TNF production and activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If anti-TNF antibodies or soluble TNF receptors are used to block TNF action, then TNF function is inhibited, but the source of TNF production remains active leading to incomplete protection and potential side effects

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidincomplete protection and side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention extracts and eliminates the source of TNF production by selectively destroying TNF-producing cells, rather than merely blocking TNF function. This is achieved through chimeric proteins that specifically target and kill the cells producing excessive TNF, removing the ongoing source of pathology.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention uses chimeric proteins as intermediary agents that combine targeting specificity with cytotoxic activity. These chimeric molecules mediate between the diagnostic need for TNF identification and the therapeutic need for cell destruction, providing a bridge between detection and elimination of the pathogenic source.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Duration of action of stationary object

If cytokine-producing cells are destroyed to prevent further cytokine synthesis, then durable protection is achieved, but systemic effects may occur

Engineering Contradiction:
Improvedurable protectionVSAvoidsystemic effects
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The invention applies local quality by making the cytotoxic agent highly specific to TNF-producing cells through the use of cell-specific targeting agents. This ensures that only the cells producing excessive TNF at specific disease sites are destroyed, while other cells throughout the body remain unaffected, thus achieving durable local protection without systemic damage.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention changes the parameter of cellular specificity by modifying the targeting mechanism to recognize unique surface markers on TNF-producing cells. This parameter change allows selective destruction of pathogenic cells while preserving normal cells, enabling durable therapy with minimized systemic effects.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If chimeric proteins are used to selectively target and destroy TNF-producing cells, then TNF production is reduced at specific sites, but the complexity of the therapeutic agent increases

Engineering Contradiction:
Improveselective targeting efficacyVSAvoidchimeric protein structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention merges multiple functional components into a single chimeric protein molecule: a cell-specific targeting agent for recognition, a translocation domain for cellular entry, and a cytotoxic effector domain for cell killing. This consolidation achieves selective targeting and destruction in one agent, balancing enhanced efficacy with manageable complexity through functional integration.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The chimeric protein structure embodies multi-functionality by incorporating domains that perform targeting, translocation, and cytotoxic activities within a single molecule. This universal design allows one agent to accomplish multiple therapeutic tasks, reducing the need for separate diagnostic and therapeutic components.

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

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 more durable protection by selectively targeting and reducing TNF production at specific sites, minimizing systemic effects and enhancing therapeutic outcomes in diseases like rheumatoid arthritis and cancer.

Implementation Method 1

connected by a translocation polypeptide, wherein the translocation polypeptide enables the chimeric protein or a fragment thereof to be translocated from the endosome to the cytosol of a target cell

Methodology Applied
Scientific EffectTranslocation:

Implementation Method 2

YopP, which has reduced or non-apoptotic activity

Methodology Applied
Scientific EffectApoptosis induction:

Implementation Method 3

YopP seems to be a protease, possibly of the de-SUMOylating family... Mutations in catalytic triad (His 109, Glu 128 and Cys 172 in YopP) disable YopP to inhibit either the MAPK or the NF-kB pathway

Methodology Applied
Scientific EffectSignal transduction inhibition:

Data Source

PatentEP1871880B8Chimeric proteins comprising yersinia yop, their preparation and pharmaceutical compositions containing them
Publication Date: 2012.09.12 YEDA RES & DEV CO LTD

AI summary

The present invention relates to a chimeric protein comprising a cell-targeting agent and a Yersinia outer protein, connected by a translocating polypeptide. The invention further relates to the preparation and use of such chimeric protein.