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Chemokine receptors are seven-transmembrane domain G-protein coupled receptors that mediate the biological activities of chemokines. Most of these receptors exhibit promiscuous binding properties whereby several different chemokines signal through the same receptor. They are named according to the chemokine subfamily they bind. There are currently eleven CC-specific receptors designated CCR1 to CCR11.
CCR5 plays a critical role in HIV entry into the target cells. Moreover, the CCR5 ligands macrophage inflammatory protein (MIP)-1 alpha, MIP-1 beta and RANTES act as endogenous inhibitors of HIV infection, making both CCR5 and its chemokine ligands attractive therapeutic targets for HIV infection. Recent studies have also highlighted the role of CCR5 in a variety of other human diseases, ranging from infectious and inflammatory diseases to cancer.