The chemokine receptors CCR5 and CXCR4 are the main coreceptors of the macrophage-tropic and T-cell- tropic HIV-1 strains, respectively. CCR5 antagonists (such as TAK-779 and SCH-C) and CXCR4 antagonists (such as AMD3100 and T22) can block HIV-1 entering their target cells by binding to CCR5 and CXCR4, respectively. The mechan- isms of HIV-1 binding to these two coreceptors and progress of research and development of the coreceptor antagonists are reviewed.