ABSTRACT

Receptors and enzymes constitute the majority of small-molecule drug targets. This focus may, in part, be due to the fact that many of these proteins’ functions rely on binding of small molecule natural ligands and substrates. In these cases, drug design and discovery efforts can model drugs after those small molecules. Additionally, as discussed in Chapters 6 and 7, the three-dimensional structures of receptors and enzymes have inherent features that make their function amenable to modulation by small molecules.