Target intelligence / Profile preview

C-X-C chemokine receptor 1; C-X-C chemokine receptor 2 (CXCR1 (for C-X-C chemokine receptor 1); CXCR2 (for C-X-C chemokine receptor 2))

Target
CXCR1 (for C-X-C chemokine receptor 1); CXCR2 (for C-X-C chemokine receptor 2)
Molecular classification
G protein-coupled receptor (GPCR), Rhodopsin-like Class A GPCR subfamily, Chemokine receptor
01

Overview

CXCR1 and CXCR2 are **class A G protein-coupled receptors** located on the plasma membrane of leukocytes and other cell types. They bind ELR+ CXC chemokines (primarily CXCL8/IL-8 for CXCR1 and CXCL1, CXCL2, CXCL3, CXCL5, CXCL6, CXCL7, CXCL8 for CXCR2)[1][2]. These receptors transduce signals that recruit and activate neutrophils during infection and inflammation, and also play roles in endothelial cell function, angiogenesis, and tumorigenesis. CXCR1 has a preference for monomeric chemokines, while CXCR2 binds both monomeric and dimeric forms, reflecting differences in their structure and ligand interaction[5]. Both receptors are highly conserved in vertebrates and are localized adjacent on chromosome 2q34-q35[1]. Their targeting has therapeutic promise in cancer, chronic inflammation, and infection, but also poses safety risks due to interference with host defense mechanisms[2][6].

Other names
IL-8 receptor Ainterleukin-8 receptor AIL8RACD181IL-8 receptor Binterleukin-8 receptor BIL8RBCD182IL-8 receptorsELR+ chemokine receptors
02

Mechanism of action

Inhibition of chemokine-induced neutrophil recruitment\nBlockade of GPCR-mediated signaling cascades (e.g., Ras/MAPK, PI3K/Akt, PLC/PKC)\nSuppression of inflammation and ROS generation by impeding CXCL8/CXCL1/CXCL2 signaling through receptor antagonism[2][4][6]

03

Biological functions

Signal transductionChemotaxis (cell movement toward chemical gradients)Immune response (especially neutrophil recruitment and activation)Angiogenesis (formation of new blood vessels)Cell proliferationCell migrationInflammatory response
04

Disease associations

Cancer (tumor growth, metastasis, angiogenesis)Inflammation (acute and chronic)Infection (bacterial clearance)Cardiovascular disease (heart tissue injury due to neutrophil recruitment)Other: autoimmune, pulmonary disease (e.g., COPD, asthma)
05

Safety considerations

Increased risk of infection (by inhibiting neutrophil trafficking)Potential impairment of normal host immune defense against pathogensOff-target immunosuppression and related complicationsPossible effects on angiogenesis and tissue repair
06

Interacting drugs

Reparixin (CXCR1/2 inhibitor)

4 more in the full profile.

07

Biomarkers

CXCL8 (IL-8) serum or tissue levelsExpression levels of CXCR1/2 in tumors or inflammatory tissuesChemokine ligand profiles (e.g., ELR+ CXC chemokines)

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