CXC chemokine receptor (CXCR) (CXCR)

CXC chemokine receptors (CXCRs) are a family of seven-transmembrane G protein-coupled receptors that play a pivotal role in the immune system by mediating the migration of leukocytes toward gradients of CXC chemokines (StatPearls, 2023). This family includes seven members (CXCR1–CXCR7), each exhibiting specific ligand preferences and tissue distributions that govern processes such as inflammation, hematopoiesis, and angiogenesis (UniProt, 2024). For example, CXCR4 is essential for the homing of hematopoietic stem cells to the bone marrow and is frequently overexpressed in various cancers, where it promotes metastasis and survival (PubMed, 2021). CXCR1 and CXCR2 are primarily involved in the recruitment of neutrophils to sites of injury or infection, making them key targets for treating chronic inflammatory conditions like COPD and rheumatoid arthritis (Nature Reviews Drug Discovery, 2019). Therapeutic strategies targeting these receptors largely involve small molecule antagonists and monoclonal antibodies designed to disrupt the chemokine-receptor axis (NIH, 2023). While Plerixafor is currently the most prominent approved CXCR4 antagonist for stem cell mobilization, numerous other candidates are in clinical development for oncology and rare genetic disorders like WHIM syndrome (X4 Pharmaceuticals, 2024).

Other names

Alpha-chemokine receptorCXC-RCXC-CKRCXC-type chemokine receptor

Antagonism of the receptor to prevent ligand binding and subsequent downstream G-protein or beta-arrestin signaling cascades, thereby inhibiting cellular migration and survival (PubMed, 2020).