Alzheimer's disease (AD) is the general neurodegenerative disease in the elderly. Alterations of microtubule associated protein tau are closely related to the onset and progression of AD. The role of tau protein in the development of AD has been a focus in the current study of AD, with an emphasis on the identification of compounds that inhibit tau protein phosphorylation and aggregate, and accelerate tau protein depolymerization. The current research status of tau protein as target of AD preventive and therapeutic drug was also reviewed.