Target intelligence / Profile preview

Chemokines and chemokine receptors

Molecular classification
G protein-coupled receptor, Cytokine, Receptor
01

Overview

Chemokines and their receptors constitute a complex signaling network of small chemotactic cytokines and G protein-coupled receptors (GPCRs) that orchestrate the migration, positioning, and activation of leukocytes throughout the body [1, 6]. This system is divided into four main subfamilies—CC, CXC, C, and CX3C—based on the spacing of conserved cysteine residues in the ligands [1, 10]. Beyond their fundamental role in immune surveillance and homeostatic cell trafficking, chemokines are critical drivers of pathological processes, including chronic inflammation, autoimmune diseases, and cancer progression [4, 7]. In oncology, the chemokine system promotes tumor cell proliferation, facilitates angiogenesis, and directs organ-specific metastasis [7, 9].}

Other names
Chemotactic cytokinesChemokine systemCC receptorsCXC receptorsC receptorsCX3C receptors7-transmembrane receptors
02

Mechanism of action

Drugs targeting this system primarily act as antagonists of G protein-coupled receptors, inhibiting the binding of chemokine ligands to their cognate receptors. Some agents function as allosteric modulators to alter receptor conformation, while monoclonal antibodies may neutralize ligands or deplete receptor-expressing cells through antibody-dependent cellular cytotoxicity.

03

Biological functions

ChemotaxisImmune responseInflammationCell migrationSignal transductionAngiogenesisWound healingLymphoid organogenesis
04

Disease associations

CancerInflammationInfectionAutoimmune diseaseCardiovascular diseaseNeurodegenerative disease
05

Safety considerations

Functional redundancy leading to therapeutic escapeIncreased susceptibility to infectionsOff-target effects due to widespread receptor expressionPotential for cardiovascular toxicityImmunosuppression
06

Interacting drugs

Maraviroc

9 more in the full profile.

07

Biomarkers

Serum CXCL12 levelsSerum CCL2 levelsSerum CXCL10 levelsCXCR4 expression on tumor cellsCCR9 expression on T cellsCCR10 expression on T cells

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