ABSTRACT

Advances in molecular biology and functional genomics have made important strides in the last few years, and new proteins are being identified at a much faster pace than ever before. As a result, the number of proteins that will serve as important therapeutic targets is expected to dramatically increase in the near future. Usually, however, the proof that these newly discovered proteins are causatively linked to a pathology that is treatable by somehow interfering with the protein's function must await the discovery of potent, selective small molecules that interfere with these events. This will mean that scientists involved in early lead discovery will face a new challenge: to rapidly provide leads (ligands, antagonists, inhibitors, etc.), that will be suitable for early proof-of-principle (POP) studies for these newly discovered proteins and thus help prioritize newly discovered targets for drug discovery programs. The leads thus generated will be optimized to identify development candidates and provide new therapeutically useful agents for clinical trials and ultimately for commercialization.