IL-6R Binding Polypeptides Optimized for Affinity and Potency
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Solution Overview
Problem
Current therapies for IL-6 related disorders, such as those involving IL-6R, often have limitations in terms of therapeutic and pharmacological properties, including binding affinity, avidity, efficacy, and potency, as well as higher costs and complexities in preparation.
Innovation Solution
Development of specific amino acid sequences and polypeptides that exhibit improved binding affinity and avidity to IL-6R, capable of partially or totally blocking the IL-6/IL-6R interaction and inhibiting signalization, with optimized sequences chosen from specific SEQ ID NOs or with minimal amino acid differences, to enhance therapeutic efficacy and reduce costs.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies for IL-6R are used, then therapeutic effect is achieved, but binding affinity and avidity are insufficient
Solution Approach 1:
The patent applies parameter changes by optimizing amino acid sequences through site-directed mutagenesis to improve binding affinity. Specific mutations in the CDR regions of the antibody sequences enhance the interaction strength with IL-6R while maintaining therapeutic efficacy, directly resolving the contradiction between achieving therapeutic effect and improving binding affinity.
2Reliability
If current therapies for IL-6R are used, then therapeutic effect is achieved, but efficacy and potency are limited
Solution Approach 1:
The patent improves efficacy and potency by modifying amino acid sequences to enhance binding characteristics. The optimized sequences demonstrate improved IC50 values and prolonged half-lives, directly increasing the therapeutic power while maintaining the desired therapeutic effect.
3Reliability
If current therapies for IL-6R are used, then treatment is provided, but costs and preparation complexity are high
Solution Approach 1:
The patent extracts and optimizes only the essential amino acid sequences (CDR regions) required for binding activity, removing unnecessary complexity from the full antibody structure. This allows for simplified production methods while maintaining therapeutic effectiveness, directly addressing the contradiction between treatment effectiveness and preparation complexity.
4Reliability
If current therapies for IL-6R are used, then treatment is provided, but binding avidity is insufficient
Solution Approach 1:
The patent creates composite antibody sequences by combining optimized CDR regions from different sources or configurations to achieve enhanced binding avidity. The composite sequences integrate beneficial amino acid motifs that collectively improve the overall binding strength to IL-6R while maintaining treatment effectiveness.
Data Source
AI summary
The present invention relates to amino acid sequences that are directed against/and or that can specifically bind Interleukin-6 Receptor (IL-6R) with improved affinity and/or avidity, and/or that have an improved efficacy and/or potency, and which are capable of (partially, or preferably totally) blocking the IL-6/IL-6R interaction and/or inhibit signalization through IL-6, IL-6R and/or the IL-6/IL-6R complex. The invention further relates to compounds or constructs, and in particular proteins and polypeptides, that comprise or essentially consist of one or more such amino acid sequences.The invention also relates to nucleic acids encoding such amino acid sequences and polypeptides, to methods for preparing such amino acid sequences and polypeptides, to host cells expressing or capable of expressing such amino acid sequences or polypeptides, to compositions, and in particular to pharmaceutical compositions, that comprise such amino acid sequences, polypeptides, nucleic acids and/or host cells, and to uses of such amino acid sequences or polypeptides, nucleic acids, host cells and/or compositions, in particular for prophylactic, therapeutic or diagnostic purposes.