Preferred Label : Dociparstat;
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 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 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 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 : 17Y5QL6ENT;
Origin ID : C217162;
concept_is_in_subset
- has_salt_form
- has_target
- is_free_acid_or_base_form_of
