Aquaporins (AQPs) are the specific channel proteins located in cell membrane for transporting water, and they play an important role in maintaining the body's water balance. AQPs are widely distributed in human tissues and organs, and their abnormal expressions are closely related to a series of diseases caused by water balance disorders. In recent years, great advances have been made in molecular researches, specific inhibitors, and targeted therapies of AQPs. In this review, we summarized the recent research progresses.