Structure, Function and Modulation of Chemokine Receptors: Members of the G-Protein-Coupled Receptor Superfamily

Chemokine receptors are membrane proteins that play an important role in inflammation and the cellular entry of human immunodeficiency virus type I (HIV-1). Understanding the structure-function relationship of chemokine receptor-ligand interactions and developing novel strategies to control these interactions have important implications for therapeutic intervention of human diseases such as HIV-1 infection. This article reviews the work carried out in our laboratory in molecular modeling and site-directed mutagenesis of chemokine receptor-ligand interactions and chemical synthesis of chemokine-derived peptide agonists and antagonists. These studies demonstrate a paradigm for exploring and controlling membrane protein-protein interactions.