Chemokine receptors control and mediate a diverse array of physiological and pathogenic processes. Many seven transmembrane (TM) G-protein-coupled receptors (GPCRs), including chemokine receptors, exist as homo- or heterodimers. Growing evidence indicates that the dimeric form is the basic functional structure of these receptors. Hetero-dimerization may allow for enhanced or specific functions of receptors and may be essential for receptor activity. Thus, dimers may provide new targets for chemokine receptor-based therapies. Synthetic peptides of TM regions of chemokine receptors may interfere with homologous interactions and inhibit functional activity of the receptors. Therefore, TM peptides and possibly compounds that target dimers and/or signaling of chemokine receptors may have therapeutic applications.