Target intelligence / Profile preview

C-C motif chemokine ligand 5 (CCL5) (CCL5)

Target
CCL5
Molecular classification
Chemokine, CC chemokine subfamily
01

Overview

CCL5, also known as RANTES, is an 8 kDa proinflammatory CC chemokine encoded by the CCL5 gene on chromosome 17q11.2-q12. It acts as a chemoattractant for various immune cells including monocytes, T cells, eosinophils, basophils, NK cells, dendritic cells, and mast cells, promoting leukocyte recruitment to inflammation sites, basophil histamine release, eosinophil activation, and NK cell proliferation. It binds primarily to CCR5 (highest affinity), and also CCR1, CCR3, CCR4, with possible activity at GPR75. CCL5 exhibits HIV-suppressive activity from CD8+ T cells by blocking R5 HIV strains via CCR5, though high levels may enhance replication. Expressed by T cells, monocytes, epithelial cells, fibroblasts, and platelets, it drives inflammation, fibrosis, angiogenesis, and tumor progression in diseases like cancer, asthma, fibrosis, and atherosclerosis

Other names
RANTESregulated on activation normal T cell expressed and secretedeosinophil chemotactic cytokineSCYA5SISdSmall Inducible Cytokine Subfamily A (Cys-Cys) Member 5
02

Mechanism of action

Chemokine receptor antagonism (e.g., CCR5 blockade by maraviroc inhibits cell migration, tumor growth, metastasis); neutralization of CCL5 (antibodies block migration, proliferation, fibrosis, angiogenesis); inhibition of HIV entry via CCR5 coreceptor blockade

03

Biological functions

Chemoattractant for monocytes, memory T-helper cells, eosinophils, T cells, basophils, NK cells, dendritic cells, mast cellshistamine release from basophilseosinophil activationHIV suppressionleukocyte recruitment to inflammation sitesNK cell proliferation and activationpossible agonist of GPR75
04

Disease associations

InflammationCancer (breast, colon, lung, ovarian, pancreatic, etc.)HIV infectionfibrosis (liver, pulmonary)atherosclerosispulmonary arterial hypertensionasthma
05

Safety considerations

High CCL5 concentrations may increase HIV replicationblockade may impair antiviral responses in chronic infections
06

Interacting drugs

Met-RANTES

4 more in the full profile.

07

Biomarkers

Elevated CCL5 levels in breast cancer tissue (3-5x higher than normal, correlates with estradiol)potential in ER+ breast cancer monitoring

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