Target intelligence / Profile preview

Chemokine C-X-C motif receptor 1 (CXCR1)

Target
CXCR1
Molecular classification
G protein-coupled receptor, Chemokine receptor, Receptor
01

Overview

Chemokine C-X-C motif receptor 1 (CXCR1) is a G protein-coupled receptor principally expressed on neutrophils and other immune cells, serving as a high-affinity receptor for the chemokine CXCL8 (also known as interleukin-8)[2][3]. Activation of CXCR1 by CXCL8 initiates intracellular signaling that promotes chemotaxis, degranulation, and other neutrophil effector functions crucial for innate immune response and inflammation[2]. CXCR1, along with the closely related CXCR2, is implicated in mediating inflammatory responses and plays a notable role in several pathological conditions, including cancer progression, infections, and chronic inflammatory diseases[2]. The receptor is a validated therapeutic target with several inhibitors studied for inflammatory and oncologic indications, though its central role in neutrophil function raises potential safety concerns regarding infection susceptibility[2][3].

Other names
Interleukin-8 receptor AIL-8RACD181C-X-C chemokine receptor type 1
02

Mechanism of action

Antagonism of receptor-mediated chemokine signaling; Blockage of G protein signaling cascade; Inhibition of neutrophil migration and activation

03

Biological functions

Immune responseSignal transductionCell migration (chemotaxis)Inflammation
04

Disease associations

CancerInflammationInfectionOther (e.g., tissue damage, autoimmune disease)
05

Safety considerations

Risk of impaired host defense (neutrophil function suppression)Potential for opportunistic infections due to immunomodulationOff-target effects impacting CXCR2 or other GPCRs
06

Interacting drugs

Reparixin

2 more in the full profile.

07

Biomarkers

CXCL8 (interleukin-8) levels for activation/stateCXCR1 expression in neutrophils or certain tumor types

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