ABSTRACT

Based on current knowledge, there are approximately 3000 genes in the human genome that code for proteins that are considered druggable; that is, capable of having their activity modulated by binding of druglike compounds. This number is expanding, however, as medicinal chemistry evolves to develop and optimize methods and strategies aimed at interfering with historically undruggable targets such as proteins that mediate physiological processes through protein–protein interactions. It has been estimated that between 600 and 1500 proteins are involved in disease processes, and the actual number of human targets of approved drugs has recently been estimated to be over 650. Target proteins that are unique to pathogens number almost 200. Of the approximately 1000 small-molecule drugs on the market, the vast majority bind to fewer, approximately 600 macromolecular targets.