Preferred Label : Ladarixin Sodium;
NCIt synonyms : Meraxin Sodium;
NCIt definition : The sodium salt form of ladarixin, an orally bioavailable, small molecule, dual inhibitor
of C-X-C motif chemokine receptors 1 (CXCR1) and 2 (CXCR2), with potential anti-inflammatory
and antineoplastic activities. Upon oral administration, ladarixin selectively targets
and allosterically binds to CXCR 1 and 2, thereby preventing CXCR1 and CXCR2 activation
by their ligand and pro-inflammatory chemokine interleukin 8 (IL-8 or CXCL8). This
inhibits CXCR1/2-mediated signaling, which inhibits inflammatory processes, reduces
both the recruitment and migration of immunosuppressive myeloid-derived suppressor
cells (MDSCs) and neutrophils in the tumor microenvironment (TME), and abrogates the
immunosuppressive-induced nature of the TME. This allows effector cells, such as natural
killer (NK) cells and cytotoxic T-lymphocytes (CTLs), to kill and eliminate cancer
cells, and inhibits tumor cell migration, metastasis, angiogenesis and tumor cell
proliferation. CXCR1 and 2, G protein-coupled receptor proteins located on myeloid
cells and certain tumor cells, play key roles in the immunosuppressive nature of the
TME, tumor metastasis, resistance to chemotherapeutic agents and myeloid cell suppression.
They also play a key role in inflammation and their expression is elevated in several
inflammatory-driven diseases.;
CAS number : 865625-56-5; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 865625-56-5
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G-SRS /a ;
Molecule name : DF-2156A; DF 2156A;
Origin ID : C200853;
concept_is_in_subset
- has_free_acid_or_base_form
- has_target
- is_salt_form_of
