Human BDCA-2 Antibody Variable Region Engineering

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Solution Overview

Problem

Current anti-human BDCA-2 antibodies are ineffective in controlling the function of plasmacytoid dendritic cells (pDCs), which are abnormally activated in autoimmune diseases like systemic lupus erythematosus, leading to excessive interferon-alpha production.

Innovation Solution

Development of a novel anti-human BDCA-2 antibody with specific amino acid sequences in its heavy and light chain variable regions, which binds to the extracellular region of BDCA-2 on pDCs, inhibiting IFNα production and controlling pDC function.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If mouse monoclonal antibody AC144 is used to inhibit pDC activation, then IFNα production is suppressed, but the antibody shows insufficient efficacy in controlling pDC function in autoimmune diseases

Engineering Contradiction:
Improveefficacy in controlling pDC functionVSAvoidexcessive IFNα production
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the antibody's species origin from mouse to human, and by optimizing the amino acid sequences in the variable regions. This creates a fully human anti-BDCA-2 antibody with enhanced binding affinity and specificity, thereby improving the reliability of pDC function control while maintaining the inhibitory effect on IFNα production.

Inventive Principle:
Principle #35Parameter changes

2Measurement precision

If existing anti-BDCA-2 antibodies are used, then some inhibition of pDC activation is achieved, but they fail to effectively bind to human BDCA-2 and control pDC function

Engineering Contradiction:
Improvebinding specificity to human BDCA-2VSAvoidfunctional control of pDCs
Core Design Contradiction:
Measurement precisionVSReliability

Solution Approach 1:

The patent applies local quality by specifically optimizing the amino acid sequences in the variable regions (VH and VL) of the antibody. By focusing modifications on these local binding regions while maintaining the overall antibody structure, the invention achieves enhanced binding specificity to human BDCA-2's extracellular domain, which directly improves both measurement precision and functional reliability.

Inventive Principle:
Principle #3Local quality

3Object-generated harmful factors

If mouse monoclonal antibodies are used against human BDCA-2, then crosslinking of BDCA-2 molecules occurs, but the therapeutic effectiveness is limited

Engineering Contradiction:
ImproveIFNα production from pDCsVSAvoidproduction of effective therapeutic antibody
Core Design Contradiction:
Object-generated harmful factorsVSEase of manufacture

Solution Approach 1:

The patent applies this principle by replacing the mouse monoclonal antibody (which has limited therapeutic utility despite being easier to produce) with a fully human antibody. The human antibody structure allows for better therapeutic compatibility and prolonged effectiveness, making it a superior disposable therapeutic agent that can be produced through standard recombinant DNA technology in human cell lines.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Data Source

PatentUS10294301B2Anti-human BDCA-2 antibody
Publication Date: 2019.05.21 ASTELLAS PHARMA INC

AI summary

[Problem] Provided is an anti-human BDCA-2 antibody for preventing or treating an autoimmune disease by binding to a human BDCA-2 to control the function of a plasmacytoid dendritic cell through human BDCA-2.[Means for Solution] The present inventors have investigated anti-human BDCA-2 antibodies, and as a result, they have provided an anti-human BDCA-2 antibody comprising a heavy chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 120 of SEQ ID NO: 2 and a light chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 109 of SEQ ID NO: 4, a heavy chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 120 of SEQ ID NO: 6 and a light chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 108 of SEQ ID NO: 8, and a heavy chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 122 of SEQ ID NO: 10 and a light chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 108 of SEQ ID NO: 12.