Protein Structures as Templates for the Design of New Drugs

Abstract

Structure-based drug design has been most commonly employed to develop enzyme inhibitors. Since the structure of the active site of an enzyme is usually well understood and relatively rigid, the act of tailoring an organic molecule to precisely fit the enzyme's active site is a technically demanding, but relatively straightforward procedure.
There is a great potential of therapeutic target proteins that are at least equally attractive as enzymes, but a perception exists that these targets are less favorable for effectively use as design templates. It is difficult to leave the well-known enzyme inhibitor research field to invest more effort in an even more challenging area, without the security of a rapid success.