Search results for "heparanase"

Microenvironment modulation and enhancement of antilymphoma therapy by the heparanase inhibitor roneparstat

2018

Anti-Metastatic Activities of Heparins

2009

Heparins are commonly administered to cancer patients for the treatment and prophylaxis of thromboembolic events. Importantly, apart from the anti-thrombotic action of these drugs, several clinical trials have demonstrated an improved survival of cancer patients who were administered low-molecular-weight heparins (LMWHs). This improved survival was independent of the anti-thrombotic efficacy, since vitamin K antagonists did not improve clinical prognosis. Moreover, this protective effect was not the result of an inhibition of the growth of primary tumors, but rather the prevention of the spreading of cancer through metastases. This has been also shown in some animal experiments. The protect…

Kinetic analysis and molecular modeling of the inhibition mechanism of roneparstat (SST0001) on human heparanase

2016

Heparanase is a β-d-glucuronidase which cleaves heparan sulfate chains in the extracellular matrix and on cellular membranes. A dysregulated heparanase activity is intimately associated with cell invasion, tumor metastasis and angiogenesis, making heparanase an attractive target for the development of anticancer therapies. SST0001 (roneparstat; Sigma-Tau Research Switzerland S.A.) is a non-anticoagulant 100% N-acetylated and glycol-split heparin acting as a potent heparanase inhibitor, currently in phase I in advanced multiple myeloma. Herein, the kinetics of heparanase inhibition by roneparstat is reported. The analysis of dose-inhibition curves confirmed the high potency of roneparstat (I…