Advancing Molecular Design
with Glycan Modification
A simple modification—adding glycans—can significantly enhance formulation properties and pharmacokinetics. This new design option improves drug performance without compromising the structure of active molecules.
The Mechanism of Simple Glycan Modification
Our glycan reagents can introduce functional groups such as primary amine, bromoacetyl, maleimide, and NHS groups at the molecular termini. This enables simple and flexible conjugation or modification with various molecules.
Examples of Available Functional Groups
Library
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Functional Benefits of Glycans
Glycans can influence key molecular properties such as water solubility, long circulation, and biocompatibility. These three attributes are critical to enhancing pharmaceutical functionality, and glycan modification offers an effective way to optimize them.
Water Solubility
The high hydrophilicity of glycans can dramatically enhance the water solubility of poorly soluble molecules.
Example 1
A glycan was conjugated to a poorly soluble peptide, and its aqueous compatibility and solubility were evaluated.
* Source: Chem. Eur. J., 2023, 31, e202300111.
* The data were obtained by GlyTech Inc.
Long Circulation
Due to their bulky structure and negative charge, glycans help reduce renal clearance, thereby increasing circulation time.
Example 2
A glycan was conjugated to the peptide hormone SRIF-28 to assess circulation time.
* Source: Chem. Eur. J., 2023, 31, e202300111.
* The data were obtained by GlyTech Inc.
Biocompatibility
Glycans are ubiquitous in biological systems and are less likely to trigger immune responses. Additionally, sialic acid residues may contribute to immunosuppressive effects, making glycan modification a promising biocompatible approach.
Example 3
A glycan was conjugated to Exendin-4 (Ex-4), a GLP-1 analogue, and the induction of anti-Ex-4 antibodies was evaluated.
* The data were obtained by GlyTech Inc.
Expanding Modalities through Glycan Engineering
The capabilities of glycan modification go beyond basic physical improvements. By combining glycans with various modalities—such as antibodies, peptides, or drug delivery systems (DDS)—more sophisticated functional designs can be achieved according to specific molecular objectives.
Antibody Drugs
The activity of antibody drugs is closely related to the structure of glycans attached to the antibodies. By adding tailored glycan structures, activity can be precisely controlled, greatly expanding the potential of antibody therapeutics.
Peptide Drugs
Peptide drugs are valued for their high target selectivity, but face challenges such as rapid degradation and frequent dosing. Glycan modification can improve protease resistance and extend circulation time, significantly enhancing their practicality.
Drug Delivery Systems (DDS)
Glycans exhibit high affinity for specific glycan receptors. Leveraging this, drugs can be delivered precisely to tumor cells or inflamed tissues. Glycan-based DDS approaches aim to maximize therapeutic effects while minimizing side effects—a dual benefit in modern medicine.
