Target intelligence / Profile preview

CC chemokine receptor 5 (CCR5)

Target
CCR5
Molecular classification
G protein-coupled receptor (GPCR), Chemokine receptor, Integral membrane protein
01

Overview

CC chemokine receptor 5 (CCR5) is a seven-transmembrane G protein-coupled receptor expressed primarily on T cells, macrophages, dendritic cells, and microglia. It mediates immune cell migration by binding several inflammatory CC chemokines such as CCL3/MIP‑1α, CCL4/MIP‑1β, and CCL5/RANTES. Beyond its physiological role in immune surveillance and inflammation, CCR5 serves as an essential co-receptor—alongside CD4—for cellular entry by macrophage-tropic strains of human immunodeficiency virus type 1 (HIV‑1). Individuals with homozygous loss-of-function mutations in the CCR5 gene are highly resistant to these forms of HIV infection but may have altered responses to other pathogens. Pharmacological inhibition or genetic disruption of CCR5 has been explored therapeutically for both infectious diseases like HIV/AIDS and chronic inflammatory conditions.

Other names
C-C motif chemokine receptor 5CD195CCR5_HUMAN
02

Mechanism of action

Antagonists block binding of endogenous chemokines or viral proteins, preventing signal transduction or viral entry into host cells. For example, maraviroc binds to CCR5 and inhibits its interaction with the HIV envelope glycoprotein gp120, thereby blocking virus-cell fusion and subsequent infection.

03

Biological functions

Signal transduction via G proteinsImmune response modulation, particularly leukocyte migration and activationChemotaxis of T cells and macrophages to sites of inflammation or infectionCo-receptor for HIV entry into host cells (with CD4)
04

Disease associations

Infection (notably HIV/AIDS as an essential co-receptor for viral entry)Inflammation/autoimmune diseaseCancer progression/metastasis in some contexts
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Safety considerations

Potential immunosuppression due to impaired leukocyte trafficking if blocked long-termRisk of increased susceptibility to other infections when using antagonists like maravirocGenetic polymorphisms may affect drug efficacy or safety profile
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Interacting drugs

Maraviroc (FDA-approved small molecule antagonist for HIV treatment)
07

Biomarkers

Presence or absence of functional CCR5 alleles can be used as a biomarker for susceptibility/resistance to HIV infection. The Δ32 mutation in the CCR5 gene confers resistance to certain strains of HIV.

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