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

C-C chemokine receptor type 1 (CCR1) and C-C chemokine receptor type 5 (CCR5) are closely related members of the G protein-coupled receptor superfamily, each possessing seven transmembrane domains and serving as key receptors for CC-class (β) chemokines such as CCL3 (MIP-1α), CCL4 (MIP-1β), and CCL5 (RANTES)[3][5][7]. These receptors are expressed on monocytes, lymphocytes, dendritic cells, mast cell progenitors, and other immune cell types, where they regulate leukocyte recruitment and trafficking during inflammatory responses[1][5]. CCR5 is also critical for HIV-1 entry into immune cells, providing a central target for antiretroviral therapies[2]. Both CCR1 and CCR5 are implicated in the pathogenesis of a range of inflammatory and autoimmune diseases, as well as in tumor microenvironment modulation and certain infectious diseases. Their therapeutic targeting mainly relies on small-molecule antagonists or antibodies that block receptor-ligand interactions, though clinical translation has been hampered by redundancy in chemokine signaling pathways, safety concerns, and the emergence of drug resistance in the context of HIV-1[4][6][8].

Other names

CD191C-C CKR-1CC chemokine receptor 1CD195C-C CKR-5CC chemokine receptor 5

Competitive antagonism or blockade of ligand binding (prevents chemokine-induced signaling); Inhibition of HIV-1 entry (CCR5 acts as a major HIV-1 co-receptor); Inhibition of inflammatory cell recruitment and tissue infiltration