Preferred Label : CXCR1/2 Inhibitor RP72;
NCIt synonyms : CXCL8 Receptor Inhibitor RP72; CXCR1/2 Inhibitor Rise Prot-72; CXCR1/CXCR2 Inhibitor RP-72; CXC chemokine receptor types 1 and 2 Inhibitor RP72; Rise Prot-72;
NCIt definition : A small molecular weight protein and an inhibitor of CXC chemokine receptor types
1 (CXCR1) and 2 (CXCR2), with potential immunomodulating, anti-inflammatory and antineoplastic
activities. Upon administration, CXCR1/2 inhibitor RP72 targets and binds to CXCR1
and CXCR2 and prevents CXCR1 and CXCR2 activation by its ligand interleukin 8 (IL-8
or CXCL8). This blocks CXCL8-mediated signal transduction and may cause cancer stem
cell (CSC) apoptosis. This may also reduce both recruitment and migration of immunosuppressive
myeloid-derived suppressor cells (MDSCs) and neutrophils in the tumor microenvironment
(TME), inhibits inflammatory processes 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. Altogether, blocking
CXCL8-mediated signal transduction may inhibit tumor cell migration, metastasis, angiogenesis
and tumor cell proliferation. CXCR1 and CXCR2, G protein-coupled receptors located
on myeloid cells and certain tumor cells, play key roles in CSC survival and the ability
of CSC to self-renew, the immunosuppressive nature of the TME, tumor cell proliferation
and metastasis, and resistance to chemotherapeutic agents.;
Molecule name : RP-72; RP 72;
NCI Metathesaurus CUI : CL1642754;
Origin ID : C176750;
UMLS CUI : C5445010;
Semantic type(s)
- concept_is_in_subset
- has_target
