Mechanism
CCR5 co-receptor
Assets acting on this target.
- Class
- CCR5 antagonist
CCR5 is a cell-surface receptor found mainly on immune cells such as T lymphocytes, macrophages, and dendritic cells. Under normal physiology it is a chemokine receptor: it binds small signaling proteins called chemokines and directs the migration of immune cells toward sites of infection or inflammation. CCR5 also serves as a co-receptor that many strains of HIV use, together with the CD4 protein, to attach to and enter host cells. Blocking CCR5 therefore prevents these viral strains from gaining entry, without directly attacking the virus itself. This approach is relevant in HIV infection, particularly for viral populations described as R5-tropic, which preferentially use CCR5 rather than the alternative co-receptor CXCR4. Because CCR5 also participates in normal immune trafficking and inflammatory signaling, interest in modulating it extends beyond infectious disease into areas where excessive immune cell recruitment contributes to tissue damage, such as certain inflammatory and fibrotic conditions, and into some oncology settings where chemokine signaling supports tumor-associated immune cell recruitment. The receptor can be targeted either with small molecules that occupy its binding pocket or with monoclonal antibodies that bind the receptor's external surface, each achieving the same functional outcome of preventing productive engagement with chemokines or viral envelope proteins.
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