2-O, 3-O Desulfated Heparin

A non-anticoagulant heparin derivative in which the 2-O and 3-O sulfate groups of heparin are removed, with potential anti-inflammatory and antineoplastic activity. Upon administration, 2-O, 3-O desulfated heparin (ODSH) prevents the interaction of the receptor for advanced glycation end-products (RAGE) to its ligands, such as advanced glycation end-products (AGEs), Mac-1(CD11b/CD18), the nuclear protein high mobility group box protein-1 (HMGB-1), carboxymethyl lysine-bovine serum albumin (CML-BSA) and members of the S100 calgranulin family. In addition, this agent inhibits the enzymes heparanase, cathepsin G, and human leukocyte elastase, which are involved in inflammation and metastasis. ODSH also inhibits selectins, thereby preventing the adhesion of tumor cells to endothelium and platelets. Altogether, this may inhibit tumor cell invasiveness and metastasis. Unlike heparin, this agent does not induce heparin-induced thrombocytopenia (HIT). RAGE, a receptor belonging to the immunoglobulin superfamily, plays a key role in inflammation and is overexpressed in a variety of cancers. (NCI Thesaurus)

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