Target intelligence / Profile preview

ELR-positive CXC chemokine (ELR+ CXC chemokine) (ELR+ CXC chemokine)

Target
ELR+ CXC chemokine
Molecular classification
Chemokine, Cytokine, Secreted protein
01

Overview

ELR-positive CXC chemokines are a specific subgroup of the CXC chemokine family defined by the presence of a conserved Glutamic acid-Leucine-Arginine (ELR) tripeptide motif at the N-terminus [12]. This group includes several potent inflammatory mediators, most notably Interleukin-8 (CXCL8), as well as CXCL1, CXCL2, CXCL3, CXCL5, CXCL6, and CXCL7 [13]. These chemokines primarily exert their biological effects by binding to and activating the G protein-coupled receptors CXCR1 and CXCR2, which are highly expressed on neutrophils [14]. Their main functions involve the recruitment and activation of neutrophils to sites of injury or infection and the promotion of angiogenesis [14]. In various diseases, such as chronic obstructive pulmonary disease (COPD), psoriasis, and many types of cancer, the overproduction of ELR+ chemokines leads to excessive tissue damage and supports tumor growth and metastasis [15]. Therapeutic strategies targeting this group include the development of monoclonal antibodies to neutralize specific ligands like IL-8 or small molecule antagonists that block the CXCR1 and CXCR2 receptors [16].

Other names
Neutrophil-activating chemokinesAngiogenic CXC chemokinesELR+ chemokinesCXCL8-like chemokines
02

Mechanism of action

Neutralization of ELR+ ligands to prevent receptor binding or competitive antagonism of the CXCR1 and CXCR2 receptors to block downstream signaling pathways [16].

03

Biological functions

Neutrophil chemotaxisAngiogenesisImmune responseInflammationCell migration
04

Disease associations

CancerChronic obstructive pulmonary disease (COPD)PsoriasisRheumatoid arthritisCardiovascular disease
05

Safety considerations

Neutropenia [9]Increased risk of bacterial infection [10]Impaired wound healing [11]
06

Interacting drugs

Reparixin

4 more in the full profile.

07

Biomarkers

Serum Interleukin-8 (IL-8) levels [6]Sputum neutrophil counts [17]CXCR2 receptor occupancy [18]

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