Peptidyl IL-2Rα Ligands for Selective Receptor Modulation

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Solution Overview

Problem

Current therapies for cancer and autoimmune diseases lack effective targeting and modulation of the IL-2 receptor (IL-2R) signaling pathway, which is crucial for immune response and tolerance.

Innovation Solution

Development of peptidyl IL-2Rα ligands that bind specifically to the human IL-2Rα subunit with high affinity, enabling targeted activation or inhibition of IL-2R for therapeutic applications, including cancer treatment and autoimmune disease management.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies are used for cancer and autoimmune diseases, then treatment is provided, but effective targeting and modulation of the IL-2R signaling pathway is lacking

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtargeting capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention segments the IL-2 receptor complex by developing compounds that specifically target the IL-2Rα subunit independently. This allows selective modulation of IL-2R signaling through the α-subunit, enabling targeted therapy that can distinguish between different IL-2R signaling contexts (cancer vs. autoimmune diseases) by acting on a specific component of the receptor complex rather than requiring whole-receptor targeting

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The peptidyl IL-2Rα ligands act as intermediary molecules that bind specifically to the IL-2Rα subunit. These compounds serve as mediators between the therapeutic goal (modulating IL-2R signaling) and the biological target (IL-2Rα), providing a controlled interface for therapeutic intervention that enables both activation and inhibition strategies

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If peptidyl IL-2Rα ligands are developed to bind specifically to IL-2Rα subunit, then targeted activation or inhibition is enabled, but complexity of compound design increases

Engineering Contradiction:
Improvetargeting capabilityVSAvoidcompound design complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The invention applies parameter changes by systematically modifying peptide sequences to optimize binding affinity and selectivity for the IL-2Rα subunit. By varying amino acid parameters (sequence composition, length, post-translational modifications), the compounds achieve specific targeting capability while managing design complexity through structured optimization approaches

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The peptidyl ligands represent composite structures combining natural amino acid sequences with modified residues or conjugated moieties. This composite approach enables enhanced binding properties and targeted activity while managing complexity through modular design principles where peptide cores are systematically optimized

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

The peptidyl IL-2Rα ligands provide a means to selectively modulate IL-2R activity, enhancing therapeutic efficacy in treating diseases associated with IL-2R signaling, offering targeted approaches for both cancer and autoimmune disorders.

Implementation Method 1

peptidyl IL-2Rα ligands that bind specifically to the human IL-2Rα subunit with high affinity

Methodology Applied
Scientific EffectSpecific binding: Absorption (physical)

Data Source

PatentUS11692009B2IL-2alpha receptor subunit binding compounds
Publication Date: 2023.07.04 MEDIKINE INC

AI summary

Peptidyl IL-2Rα ligands and compounds comprising the IL-2Rα ligands are disclosed. The IL-2Rα ligands and compounds such as synthetic monomers, homodimers, or heteromers and recombinant fusion proteins comprising the IL-2Rα ligands can be used as targeting or imaging agents, as diagnostics or to treat cancers and autoimmune diseases.