Direct methods for modulating protein function

During the past few years, the drug discovery process has shifted from a chemistry- to a biology-driven paradigm. Genome sciences have made a significant contribution to this shift, leading to a plethora of potential drug targets that are mainly proteins. Genetic methods will continue to be used to characterize proteins, but more direct methods are needed to determine the suitability of these protein targets for pharmacological intervention. In addition to the use of antibodies and aptamers, technologies focusing on the direct modulation of protein activity, including chemical genetics, analog-sensitive enzyme alleles and chromophore-assisted laser inactivation, should significantly contribute to the field of post-genomic drug discovery and development.