Preferred Label : Dociparstat sodium;
NCIt synonyms : ODSH; PGX-ODSH; O-desulfated Heparin; 2,3-o-Desulfated Heparin (12000 da);
NCIt definition : A heparin derivative in which the 2-O and 3-O sulfate groups of heparin are removed
and that lacks anticoagulant activity, with potential anti-inflammatory, immodulatory
and antineoplastic activities. Upon administration, dociparstat sodium binds to both
chemokine stromal cell-derived factor 1 (SDF-1 or CXCL12) and CXC chemokine receptor
4 (CXCR4). This prevents the interaction of CXCL12 with CXCR4, blocks CXCR4 activation,
and may result in decreased proliferation and migration in CXCR4-overexpressing tumor
cells. In addition, inhibition of CXCL12/CXCR4 interaction may induce mobilization
of hematopoietic cells from the bone marrow into the blood. In addition, dociparstat
sodium prevents the interaction of the receptor for advanced glycation end-products
(RAGE) with its ligands, including advanced glycation end-products (AGEs), Mac-1(CD11b/CD18),
the nuclear pro-inflammatory 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. Altogether, this may
inhibit tumor cell invasiveness and metastasis. Dociparstat sodium also binds to platelet
factor 4 (PF4 or CXCL4) and may prevent PF4's inhibitory effect on platelet production.
This may increase platelet production. 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. CXCR4 is a chemokine receptor belonging to the G protein-coupled receptor
(GPCR) family that plays an important role in chemotaxis, chemoresistance and angiogenesis,
and is upregulated in several tumor cell types. The interaction between CXCL12/CXCR4
induces retention of hematopoietic cells in the bone marrow.;
UNII : 4O75889WF4;
CAS number : 177021-00-0;
Molecule name : PGX-100; CX-01; CX 01;
Origin ID : C99130;
UMLS CUI : C3274551;
False automatic mappings
- Semantic type(s)
- Validated automatic mappings to NTBT
- concept_is_in_subset
- has_target
