Many drugs target proteins that function as receptors for small-molecule ligands. These ligands bind to and alter the structures of their protein targets, thus modulating their biological activities. Key protein targets in the fields of biology and pharmaceutical research include the nuclear receptors (NRs) that belong to the superfamily of ligand-dependent transcription factors, the G-protein coupled receptors (GPCRs), and protein kinases, which are part of a large family of regulatory proteins.