Modified Serp-1 Protein PEGylation for Immune Modulation

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Solution Overview

Problem

Current treatments for inflammatory and immune disorders often have limited effectiveness and are associated with significant side effects, and there is a need for improved systemic and locally delivered immune modulating compositions that can target the source of inflammation without adverse effects on normal physiology.

Innovation Solution

Development of modified Serp-1 proteins with therapeutic enhancing moieties such as PEGylation to enhance pharmacokinetics, stability, and activity, allowing for systemic delivery with focused effects and reduced toxicity, while maintaining immune modulating properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for inflammatory and immune disorders are used, then immune modulation is achieved, but significant side effects occur and effectiveness is limited

Engineering Contradiction:
ImproveeffectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the Serp-1 protein by introducing therapeutic enhancing moieties such as PEGylation to alter its pharmacokinetic parameters, stability, and activity. This changes the physical and chemical properties of the protein to improve its therapeutic profile while reducing side effects

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite structure by combining Serp-1 protein with therapeutic enhancing moieties (such as PEG chains). This composite approach integrates the immune modulating properties of Serp-1 with the pharmacokinetic benefits of the attached moieties, achieving both effectiveness and reduced toxicity

Inventive Principle:
Principle #40Composite materials

2Reliability

If Serp-1 protein is used for immune modulation, then therapeutic effects are achieved, but half-life and stability are insufficient

Engineering Contradiction:
Improvetherapeutic effectsVSAvoidhalf-life
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent introduces therapeutic enhancing moieties to Serp-1 protein to fundamentally change its pharmacokinetic parameters, particularly extending its half-life and improving stability in circulation, thereby maintaining therapeutic effects for longer durations

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

By extending the half-life of Serp-1 through PEGylation and other modifications, the patent ensures continuous therapeutic action over an extended period, reducing the frequency of dosing and maintaining stable immune modulation

Inventive Principle:
Principle #20Continuity of useful action

3Reliability

If Serp-1 protein is delivered systemically, then immune modulation is achieved, but toxicity increases

Engineering Contradiction:
Improveimmune modulationVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the surface properties and charge characteristics of Serp-1 through PEGylation and other therapeutic enhancing moieties to reduce non-specific interactions with healthy tissues, thereby lowering toxicity while preserving immune modulating effects

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The therapeutic enhancing moieties act as intermediaries between the Serp-1 protein and the biological system, reducing direct toxic interactions while allowing the protein to maintain its immune modulating function through its active site

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS20230173080A1Composition of immunomodulating serpin, serp-1
Publication Date: 2023.06.08 SERPASS BIOLOGICS INC
  • US20230173080A1 patent drawing
  • US20230173080A1 patent drawing
  • US20230173080A1 patent drawing

AI summary

Disclosed herein, in some embodiments, are modified Serp-1 proteins. The modified Serp-1 protein may include a therapeutic enhancing moiety, and be biologically active. In some cases, the therapeutic enhancing moiety is a water soluble polymer such as polyethylene glycol.