ABSTRACT
Pharmacoproteomics refers to the discovery and use of protein markers for disease diag-
nosis, toxicology, drug efficacy, and patient prognosis. Although these activities are by no
means new to biomedical research, a number of developments have made possible the
global analysis of proteins direct from diseased tissues or body fluids. These advances
are predicted to yield unprecedented information about the effects of disease and
pharmaceutical intervention on the entire set of naturally existing proteins, that is, the pro-
teome, leading to the discovery of better indicators for disease treatment and drug
development. The field of proteomics is currently undergoing rapid development and,
although considerably less comprehensive and structured than, say, genomic microarray
technology, nevertheless has significantly benefited from the advances in computer
programming and data management applied to genomics. The coupling of these develop-
ments with the entire drug discovery process is now seen in most major pharmaceutical
companies, many of which have large, dedicated pharmacogenomic and transcriptomic
departments. Although proteomics is being used increasingly in drug discovery, lack of
standardization and the need for greater efficiency means that it has not yet been incorpor-
ated to the same degree as the other “-omics” fields. In this chapter, the emerging field of
pharmacoproteomics will be discussed in terms of the historical perspective of protein
targets and markers, and, where current needs may be met by proteomics, followed by
a description of existing and emerging protein discovery technologies.