Target intelligence / Profile preview

C-C chemokine receptor type 1, 3, and 5 (CCR1/CCR3/CCR5)

Target
CCR1/CCR3/CCR5
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The C-C motif chemokine receptor partners for CCL5 (RANTES) primarily include C-C chemokine receptor type 1 (CCR1), type 3 (CCR3), and type 5 (CCR5), which are members of the G protein-coupled receptor (GPCR) family (NIH, 2026). These receptors are expressed on various immune cells, including T lymphocytes, monocytes, macrophages, and eosinophils, where they mediate the chemotactic effects of CCL5, directing cells to sites of inflammation and infection (MDPI, 2023). CCR5 is particularly notable as a major co-receptor for HIV-1 entry into host cells, and its genetic deficiency (CCR5-delta32) confers resistance to infection (Frontiers, 2024). Beyond infectious disease, the CCL5-receptor axis plays a critical role in chronic inflammatory conditions such as rheumatoid arthritis, atherosclerosis, and multiple sclerosis, as well as in cancer progression and metastasis (NIH, 2025). Therapeutic strategies targeting these receptors include small molecule antagonists like Maraviroc, which is approved for HIV treatment, and dual antagonists like Cenicriviroc, which target both CCR1 and CCR5 to address inflammatory and fibrotic conditions (Patsnap, 2024).

Other names
RANTES receptorsCCL5 receptorsC-C motif chemokine receptor 1C-C motif chemokine receptor 3C-C motif chemokine receptor 5CCR1CCR3CCR5
02

Mechanism of action

Antagonism of C-C motif chemokine receptors to block the binding of CCL5 and other ligands, thereby inhibiting downstream signaling pathways such as PI3K/Akt and MAPK/ERK and preventing immune cell recruitment or viral entry.

03

Biological functions

Immune responseSignal transductionCell migrationChemotaxisInflammation
04

Disease associations

InfectionInflammationCancerAutoimmune diseaseCardiovascular disease
05

Safety considerations

Increased susceptibility to West Nile Virus infectionPotential for HIV-1 tropism shift to CXCR4Hepatotoxicity (associated with certain antagonists)Redundancy in chemokine signaling potentially limiting efficacy
06

Interacting drugs

Maraviroc

6 more in the full profile.

07

Biomarkers

CCR5-delta32 mutationCCL5 serum levelsCCR5 cell surface expressionHIV-1 viral load

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