G Protein-coupled receptors are a group of drug targets with important physiological functions and of pathological significance.In order to screen desirable drugs for the target receptors from a large amount of chemicals,high throughput screening systems with specificity and sensitivity are needed.The eukaryotic cell of Saccharomyces cerevisiae is appropriate for high throughput screening because of its advantages,including convenience of genetic manipulation,inexpensive culturing conditions,thorough understanding of its genome,sufficient tools for expressing heterologous proteins,and developed assays for detecting and analyzing.This review discusses the application and development of G protein-coupled receptors expressed in Saccharomyces cerevisiae as high throughput screening.