The events that lead to an inflammatory response are characterized by recognition of the site of injury by inflammatory cells, specific recruitment of subpopulations of leukocytes into tissue, removal of the offending agent and "debridement" of the injured cells/tissue, and repair of the site of injury with attempts to reestablish normal parenchymal, stromal, and extracellular matrix relationship. The molecular regulation of this complex physiologic process involves the interaction between cell surface, extracellular matrix, and soluble mediators, such as chemokines. Chemokine activities are mediated through G-protein coupled receptors. This is the largest known family of cell-surface receptors, which mediate transmission of stimuli as diverse as hormones, peptides, glycopeptides, and chemokines. In this review, we will focus on the signaling pathways involved in the production and function of chemokines as they relate to the inflammatory response.