Glycomimetic Ligands Modulating Siglec Receptors
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Solution Overview
Problem
There is a need for improved compositions and methods to modulate sialic-acid binding self-associated pattern recognition receptors, such as Siglecs, for treating diseases resulting from acute, chronic, or aberrant immune system activation.
Innovation Solution
The development of compounds and particles that can agonize, block, or antagonize specific Siglec receptors, using modified glycans and biocompatible polymers, to modulate immune responses and treat various diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional sialic-acid binding ligands are used, then binding to Siglec receptors is achieved, but the ability to effectively modulate immune responses for disease treatment is limited
Solution Approach 1:
The patent modifies sialic-acid binding ligands by changing chemical parameters - introducing specific molecular structures (formulas S-1, S-2, D-1, D-2) with varied R1, R, and RF groups that alter binding affinity and immunomodulatory activity, enabling effective treatment across different disease states
Solution Approach 2:
The invention creates composite particles combining ligands (formulas S-1, S-2, D-1, D-2) with biocompatible polymers (PLGA, PLuronic, poloxamer, chitosan, hyaluronic acid, heparin, polysialic acid) to achieve both targeted Siglec binding and enhanced pharmacokinetic properties for diverse therapeutic applications
2Reliability
If specific Siglec receptors are targeted, then immune response modulation is achieved, but development of compounds and particles becomes complex
Solution Approach 1:
The patent divides the ligand structure into distinct functional segments - a sialic-acid binding core (formulas S-1, S-2, D-1, D-2) and variable R1, R, and RF groups that can be independently optimized for different Siglec subtypes, allowing systematic development of specific inhibitors
Solution Approach 2:
The invention creates a universal particle platform where the same biocompatible polymer core can be conjugated with different ligand variants (formulas S-1, S-2, D-1, D-2) to target multiple Siglec receptors, enabling one platform to address multiple disease states
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compositions effectively modulate immune responses, providing treatment options for diseases such as cancer, immune-related, and inflammatory disorders by targeting Siglec receptors.
Implementation Method 1
modulating sialic-acid binding self-associated pattern recognition receptors, known as sialic-acid-binding immunoglobulin-type lectins (Siglecs)
Implementation Method 2
self-associated pattern recognition receivers
Data Source
AI summary
Described herein are glycan compounds and particles comprising glycan compounds. The compounds and particles described herein are useful in methods of treating immune and inflammatory-related diseases. or a pharmaceutically acceptable salt thereof