Preferred Label : Ladarixin;
NCIt definition : 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.;
UNII : DEH7Q6472O;
InChIKey : DDLPYOCJHQSVSZ-SSDOTTSWSA-N;
CAS number : 849776-05-2;
NCI Metathesaurus CUI : CL1382334;
Origin ID : C170087;
UMLS CUI : C4550238;
Currated CISMeF NLP mapping
- Semantic type(s)
- concept_is_in_subset
- has_salt_form
- has_target
- is_free_acid_or_base_form_of
