C5-Binding Polypeptide Sequence Modifications for Stable Activity

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Solution Overview

Problem

Existing C5 binding polypeptides suffer from stability issues, which affect their efficacy in therapeutic applications, despite retaining biological activity such as binding affinity for human complement component 5 (C5) and inhibition of the complement pathway.

Innovation Solution

Modifying specific amino acid residues in the C5 binding polypeptides, particularly at positions 52 and 53, and optionally at position 60, improves stability while maintaining biological activity, including binding affinity for C5 and inhibition of the complement pathway.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If C5 binding polypeptides are used for therapeutic applications, then binding affinity for C5 and inhibition of complement pathway is achieved, but stability is insufficient

Engineering Contradiction:
ImprovestabilityVSAvoidtherapeutic efficacy
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies parameter changes by modifying specific amino acid residues at positions 52 and 53 in the C5 binding polypeptide sequence. These sequence modifications alter the physical-chemical parameters of the polypeptide, resulting in improved stability while preserving the binding affinity for C5 and therapeutic efficacy in inhibiting the complement pathway.

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If amino acid residues are modified to improve stability, then stability increases, but biological activity may be affected

Engineering Contradiction:
Improvepolypeptide stabilityVSAvoidbiological activity
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent applies local quality by making targeted modifications at specific local positions (amino acid residues 52 and 53) within the polypeptide sequence. These localized changes improve overall stability without disrupting the critical binding regions, thereby maintaining biological activity including C5 binding affinity and complement pathway inhibition.

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP3811961B1Stable polypeptides binding to human complement c5
Publication Date: 2025.08.20 IPC RESEARCH LLC
  • EP3811961B1 patent drawingFigure 1
  • EP3811961B1 patent drawingFigure 2~3D
  • EP3811961B1 patent drawingFigure 4~5

AI summary

The invention relates to a polypeptide capable of binding human complement component 5 (C5), said polypeptide comprising the amino acid sequence [BM]-[L2]-QSX42X43LLX46EAKKLX52X53X54Q wherein [BM] is a C5 binding motif; [L2] is an interconnecting loop; X42 is selected from A and S; X43 is selected from N and E; X46 is selected from A, S and C; X52 is selected from E, N and S; X53 is selected from D, E and S, provided that X53 is not D when X52 is N; and X54 is selected from A and S.