Chemokine receptors, or CCRs, are cytokine receptors that can be found on the surface of some cells and interact with specific chemokines. Mammals have 19 different chemokine receptors that have been identified. They are all members of a large protein family known as G protein-coupled receptors because they each have a 7-transmembrane (7TM) structure and couple to G-protein for signal transduction inside of a cell. Chemokine receptors cause an increase in intracellular calcium (Ca2+) ions after interacting with their particular chemokine ligands (calcium signaling).Cell responses result from this, and one of them is the beginning of the chemotaxis process, which directs the cell to the desired area of the organism. The four different subfamilies of chemokines that chemokine receptors bind are grouped into four families: CXC chemokine receptors, CC chemokine receptors, CX3C chemokine receptors, and XC chemokine receptors. Some chemokine receptors act as entry points for HIV, while others support inflammatory conditions and cancer.
|Maraviroc (also known as UK-427857)is a potent, selective and non-competitive CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively.
|RS-504393 is a potent and highly selective CCR2 chemokine receptor antagonist with IC50s of 98 nM and > 100 µM for inhibition of human recombinant CCR2b and CCR1 receptors respectively.