EC Number   |
Application |
Reference |
|---|
   3.2.1.166 | analysis |
a simple, accurate, and robust biochemical assay for heparanase activity that uses a commercially available homogeneous substrate (fondaparinux) with a single enzymatic cleavage point and, thus, does not have the problems associated with using heparan sulfate-based assays. The assay is suitable for testing heparanase inhibitors and could easily be adapted for use in high-throughput screening applications |
701675 |
| 3.2.1.166 | diagnostics |
upregulation of heparanase expression correlates with increased tumor size, tumor angiogenesis, enhanced metastasis and poor prognosis. Heparanase expressed by tumor cells, innate immune cells, activated endothelial cells as well as other cells of the tumor microenvironment is a master regulator of the aggressive phenotype of cancer and an important contributor to the poor outcome of cancer patients |
753404 |
| 3.2.1.166 | drug development |
heparanase inhibitors used in tandem with chemotherapeutic drugs overcome initial chemoresistance, providing a strong rationale for applying anti-heparanase therapy in combination with conventional anti-cancer drugs. Heparin-like compounds that inhibit heparanase activity are being evaluated in clinical trials for various types of cancer. Heparanase expressed by tumor cells, innate immune cells, activated endothelial cells as well as other cells of the tumor microenvironment is a prime target for therapy |
753404 |
| 3.2.1.166 | drug development |
heparanase is an important target for anti-cancer and anti-inflammatory drug discovery |
731254 |
| 3.2.1.166 | drug development |
overexpression of hepaxadranase in cancers is well known and is associated with angiogenesis, inflammation and increased metastatic potential, making this enzyme a promising drug target |
754818 |
| 3.2.1.166 | drug development |
the emerging role of heparanase in tumor initiation, growth, metastasis, and chemoresistance is well recognized and is encouraging the development of heparanase inhibitors as anticancer drugs for humans |
755259 |
| 3.2.1.166 | drug development |
the enzyme is a very attractive target in drug discovery |
731425 |
| 3.2.1.166 | drug development |
the natural heparan sulfate-heparanase interactions are used as a template for the design of heparan sulfate-mimicking glycopolymers |
753249 |
| 3.2.1.166 | drug development |
the upregulation of heparanase expression increases tumor size, angiogenesis, and metastasis, represents a validated target in the anti-cancer field. 2-(4-(4-(bromo-methoxybenzamido)benzylamino)phenyl) benzazole derivatives act as anti-heparanase agents, proposing this scaffold for development of broadly effective heparanase inhibitors. Symmetrical 2-aminophenyl benzazolyl-5-acetate derivatives, proving that symmetrical compounds, are more effective than asymmetrical analogues |
754394 |
| 3.2.1.166 | medicine |
heparanase-1 is an approach towards developing new therapeutics suitable for the treatment of cancer or inflammatory diseases. The identification of only a single predominant functional heparanase suggests that if its activity can be inhibited, other heparanases may not be available to cover for it. Heparanase-inhibiting compounds might interfere with physiological processes such as wound healing and tissue-repair |
693320 |
