ABSTRACT

The pharmaceutical and biotechnology industries have encountered increasing research and development costs while facing a decreasing number of new molecular entities [1]. Even though the explosion of genomics-based drug discovery approaches has led to a large collection of potential drug targets, culling the “druggable” targets from the potential ones is the real challenge. Although the drug-discovery process is different for each company, several common steps are used within the industry. These steps include target identification and validation; lead identification and validation; and preclinical studies, with the ultimate goal of successful clinical studies (fig. 1.1). The identification and validation of targets for the pharmaceutical and biotechnology industries are complex processes that include laboratory techniques, outsourcing approaches, and informatics methodologies. However, some basic issues are addressed before a target is even selected for screening. These issues include such topics as how a target’s RNA expression correlates with protein expression and a disease hypothesis, how a target is involved in a metabolic pathway or molecular interaction network, whether a target is druggable, and how a target’s genomic locus can be correlated with a genetic marker. Of course, the challenges of target identification and validation can be accelerated using in silico technologies.