CD206-Targeting Peptide Compositions for M2 Macrophage Selectivity

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Solution Overview

Problem

Current methods lack specificity and efficacy in targeting tumor-associated macrophages (M2 TAMs) for therapeutic or diagnostic purposes, as existing peptides and nanobodies do not selectively bind to CD206, leading to non-specific binding to other mannose receptors and limited therapeutic outcomes.

Innovation Solution

Development of conformationally constrained peptides and peptidomimetics, such as CSPGAK, which selectively target CD206-expressing cells, and their use in compositions with detectable agents or therapeutic agents, including polymersomes, to specifically home to MRC1-expressing tumor-associated macrophages.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If existing peptides and nanobodies are used to target tumor-associated macrophages, then they can bind to mannose receptors, but they lack specificity and bind non-specifically to other mannose receptors, resulting in limited therapeutic outcomes

Engineering Contradiction:
Improvebinding specificityVSAvoidtherapeutic efficacy
Core Design Contradiction:
Measurement precisionVSReliability

Solution Approach 1:

The patent applies local quality by designing a peptide (CSPGAKVRC) with a specific amino acid sequence that targets only the CD206 mannose receptor subtype expressed on M2 tumor-associated macrophages. The peptide's unique sequence configuration enables it to distinguish and bind specifically to CD206 while avoiding other mannose receptor subtypes, thereby achieving both high binding specificity and reliable therapeutic efficacy in treating solid tumors

Inventive Principle:
Principle #3Local quality

2Productivity

If M2 TAMs are targeted for therapeutic intervention, then tumor growth and metastasis can be reduced, but the immunosuppressive microenvironment supported by M2 TAMs must be overcome

Engineering Contradiction:
Improvetumor growth inhibitionVSAvoidimmunosuppression
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent converts the harmful immunosuppressive function of M2 TAMs into a beneficial therapeutic effect by using the CSPGAKVRC peptide to selectively target and deplete these cells. The peptide's specific binding to CD206 on M2 TAMs triggers their elimination, thereby removing the immunosuppressive microenvironment that protects tumors, and simultaneously enhancing the effectiveness of anti-cancer therapies while reducing tumor growth and metastasis

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentEP3687559B1Compositions that target tumor-associated macrophages and methods of use therefor
Publication Date: 2025.11.12 SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INST
  • EP3687559B1 patent drawingFigure 1a~1d
  • EP3687559B1 patent drawingFigure 2a~2h
  • EP3687559B1 patent drawingFigure 3a~3c

AI summary

Described herein are peptides, compositions, and methods for diagnosing, detecting, imaging, monitoring, preventing, treating, or ameliorating diseases or disorders including cancer, inflammatory disorder, and autoimmune disease.