The molecular basis of human bitter taste perception is an area of intense research. Only 25 G protein-coupled receptors belonging to the hTAS2R gene family face the challenge to detect thousands of structurally different bitter compounds, most of which are plant metabolites. Since many natural bitter compounds are highly toxic, whereas others are part of our daily diets, bitter taste was crucial during evolution and still most likely affects our food selection. The article presented here addresses biosynthesis, functional analyses of TAS2Rs and TAS2R variants, as well as gustatory expression of hTAS2R genes.