The large family of functionally related chemotactic molecules involved in the migration and activation of specific leukocytes and inflammatory cells. Many of these chemotactic molecules bind to G-protein coupled receptors found in phagocytic cells, such as neutrophils, monocytes, dendritic cells, and other cell types including endothelial cells. Since these chemoattractant receptors and their ligands are involved in the regulation of various (patho)physiological responses, it has been hot topics to reveal these receptors as target molecules for the development of therapeutic agents. I want to discuss putative role of some chemoattractant receptors and their ligands for the application for the development of therapeutic agents against inflammatory diseases. Severe sepsis, a principal cause of death in intensive care units, occurs when host immune defenses fail to combat invading microbes. We found that neutrophil activation by stimulating chemoattractant receptors with small synthetic peptides protected against death by enhanced bactericidal activity and inhibition of vital organ inflammation and immune cell apoptosis in a cecal ligation and puncture (CLP) sepsis mouse model. I will also discuss a novel myeloid cell population that contribute mortality caused by bacterial infection.