We will firstly summarize the structures and signaling pathways of GPCRs, then address the reported implication of GPCRs in the pathologic process of AD, focusing on BACE1 related GPCRs, and also discuss the current findings on the regulatory roles of GPCRs in the pathological progression of AD, as well as the implication of GPCRs for pharmaceutical treatment of AD patients. This evidence concerns the gene BACE1 and Alzheimer disease.