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CXCR7, also known as ACKR3, is a seven-transmembrane G protein-coupled receptor (GPCR) that primarily binds the chemokines CXCL12 and CXCL11. Unlike classical chemokine receptors, CXCR7 does not signal through G proteins but instead acts mainly as a scavenger or decoy receptor, modulating the availability of its ligands and influencing cell migration, immune responses, and tumor biology. It recruits β-arrestin rather than activating traditional G-protein signaling pathways, leading to downstream activation of ERK/MAPK pathways. It is upregulated during pathological inflammation and in various cancers and is therefore a target for cancer therapy and neuroinflammatory diseases.
CXCR7 antagonists aim to block the receptor's interaction with its ligands (CXCL12 and CXCL11), preventing its scavenging activity and subsequent downstream signaling.
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