Chemoattractant receptors are a group of seven transmembrane, G protein coupled receptors (GPCRs). They were initially identified mainly on leukocytes to mediate cell migration in response to pathogen or host-derived chemotactic factors. During the past decade, chemoattractant GPCRs have been discovered not only to mediate leukocyte chemotaxis thus promoting innate and adaptive host immune responses, but also to play essential roles in development, homeostasis, HIV infection, angiogenesis and wound healing. A growing body of evidence further indicates that chemoattractant GPCRs contribute to tumor growth, invasion, angiogenesis/angiostasis and metastasis. The diverse properties of GPCRs in the progression of malignant tumors have attracted intense interest in their potential as novel anti-tumor pharmacological targets.