Target intelligence / Profile preview

Chemokine Receptor CXCR7 (CXCR7)

Target
CXCR7
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

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.

Other names
ACKR3RDC1GPR159
02

Mechanism of action

CXCR7 antagonists aim to block the receptor's interaction with its ligands (CXCL12 and CXCL11), preventing its scavenging activity and subsequent downstream signaling.

03

Biological functions

Scavenging/degradation of chemokinesModulation of chemokine gradient formationCell migrationImmune responseSignal transduction
04

Disease associations

Cancer progressionCancer metastasisNeuroinflammationMultiple sclerosisHIV-associated brain pathology
05

Safety considerations

Potential for off-target effects due to the broad expression of chemokines and their receptors.Complex role in both promoting and suppressing inflammation, requiring careful consideration of the specific disease context.
06

Interacting drugs

ACT-1004-1239

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