Bitter taste in mammals is achieved by a family of approximately 30 bitter taste receptor genes. The main function of bitter taste is to protect the organism against the ingestion of, frequently bitter, toxic food metabolites. The field of taste research has advanced rapidly during the last several years. This is especially true for the G-protein-coupled-receptor-mediated taste qualities, sweet, umami, and bitter. This review summarizes current knowledge of bitter taste receptor gene expression, signal transduction, the structure—activity relationship of bitter taste receptor proteins, as well as their variability leading to a high degree of individualization of this taste quality in mammals.