Bitter taste receptor T2R1 is activated by dipeptides and tripeptides

► Food protein derived bitter TRIPEPTIDES activate the human bitter receptor T2R1. ► Peptides with ACE-inhibitory activity were also able to activate the T2R1 receptor. ► Molecular modeling studies show T2R1 receptor has one binding site for agonist ligands. ► We identify amino acid residues on T2R1 important for ligand binding.