Target intelligence / Profile preview

Heparan sulfate glycosaminoglycan (HS-GAG) (HS-GAG)

Target
HS-GAG
Molecular classification
Glycosaminoglycan, Polysaccharide, Extracellular matrix component
01

Overview

Heparan sulfate glycosaminoglycans (HS-GAGs) are complex, linear polysaccharides found on the cell surface and within the extracellular matrix of almost all animal tissues (Source: NCBI Bookshelf, Essentials of Glycobiology, 2017). They consist of repeating disaccharide units that undergo extensive enzymatic modification, creating highly sulfated regions that serve as docking sites for a vast array of proteins, including growth factors, chemokines, and morphogens (Source: Journal of Biological Chemistry, 2015). By modulating these interactions, HS-GAGs play a critical role in regulating cell signaling, proliferation, and tissue morphogenesis (Source: Nature Reviews Molecular Cell Biology, 2007). In disease states, HS-GAGs are often exploited by pathogens for cell entry or are dysregulated in cancer to promote angiogenesis and metastasis (Source: Antiviral Research, 2020; Frontiers in Oncology, 2019). Therapeutic strategies targeting HS-GAGs include the use of heparin mimetics to block protein-GAG interactions or inhibitors of heparanase, the enzyme responsible for HS degradation, to stabilize the extracellular matrix and inhibit tumor progression (Source: Glycobiology, 2020).

Other names
Heparan sulfateHSHeparan sulphateHeparan sulfate chainsHS-GAG
02

Mechanism of action

Competitive inhibition of ligand binding to endogenous heparan sulfate and inhibition of heparanase-mediated chain cleavage (Source: Matrix Biology, 2014).

03

Biological functions

Signal transductionCell adhesionGrowth factor sequestrationViral entry mediationBlood coagulation regulation
04

Disease associations

CancerInfectionInflammationNeurodegenerative diseaseMucopolysaccharidosis
05

Safety considerations

Risk of hemorrhageThrombocytopeniaInterference with systemic growth factor signaling
06

Interacting drugs

Muparfostat

4 more in the full profile.

07

Biomarkers

Urinary heparan sulfateHeparanase activityHeparanase expression

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