C-X-C chemokine receptor family (CXCR) (CXCR)

The C-X-C chemokine receptor (CXCR) family consists of seven primary G protein-coupled receptors (CXCR1–CXCR7) that mediate the biological effects of CXC chemokines [1.1.1, 1.1.3]. These receptors are essential regulators of leukocyte trafficking, directing immune cells to sites of inflammation, infection, and tissue injury [1.1.4, 1.2.5]. Beyond their role in the immune system, CXCR members are involved in critical physiological processes such as angiogenesis, hematopoiesis, and embryonic development [1.3.1, 1.3.2]. In various diseases, the CXCR axis is often dysregulated; for example, CXCR4 serves as a major co-receptor for HIV-1 entry and is frequently overexpressed in cancers, where it facilitates tumor cell survival and metastasis to distant organs [1.2.1, 1.2.2]. Consequently, the CXCR family has become a significant focus for drug development, with several small molecule antagonists approved or in clinical trials for treating conditions ranging from stem cell mobilization and cancer to chronic inflammatory diseases [1.1.2, 1.3.3].

Other names

CXC chemokine receptorsCXCRsCXC receptorsCD181CD182CD183CD184CD185CD186ACKR3IL8RAIL8RBGPR9FusinBLR1BONZOCXCR family chemokine receptors

Antagonism of the receptor to block the binding of CXC chemokines (e.g., CXCL12, CXCL8), thereby inhibiting downstream G-protein signaling pathways such as PI3K/Akt and MAPK, which prevents cell migration, survival, and viral entry [1.2.1, 1.2.2].