C-X-C motif chemokine receptor 2 (CXCR2) (CXCR2)

C-X-C motif chemokine receptor 2 (CXCR2) is a G protein-coupled receptor (GPCR) that plays a central role in the recruitment and activation of neutrophils during inflammatory and immune responses [4, 5, 12]. It is activated by a group of "ELR+" CXC chemokines, including CXCL1 through CXCL8, which are characterized by a conserved Glu-Leu-Arg motif [5, 14, 15]. In addition to its physiological role in host defense, the CXCR2 axis is frequently implicated in the pathogenesis of chronic inflammatory diseases such as COPD and asthma, as well as in the progression of various cancers [1, 4, 16]. In the tumor microenvironment, CXCR2 signaling promotes angiogenesis and the recruitment of myeloid-derived suppressor cells (MDSCs), which contribute to immune evasion and metastasis [2, 3, 5]. Therapeutic strategies targeting CXCR2 primarily involve small-molecule antagonists and allosteric modulators, such as navarixin and reparixin, which aim to block ligand-induced signaling [4, 12, 14]. However, a major clinical challenge in targeting CXCR2 is the risk of treatment-induced neutropenia, which can compromise the patient's ability to fight infections [12, 14].

Other names

CD182IL8RBIL8R2CDw128bInterleukin 8 receptor betaGRO/MGSA receptor

Antagonism or allosteric modulation of the CXCR2 receptor to inhibit ligand-induced signaling and neutrophil recruitment.