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S C I E N T I F I C R E V I E W 1 3 Stay on track in drug discovery Growing impact of Biacore on drug discovery Keeping on schedule Reshaping assays Evaluating hits Joseph P Gardner Scientist Pfizer Inc USA the Biacore system was a key contributor to keeping the project on schedule The contributions from Biacore technology continue to have a widening impact on all aspects of the drug discovery process in today s pharmaceutical industry As biosensor technology became a practical reality in the laboratory during the early 1990s it was readily accepted by the scientific community as a powerful analytical technique for evaluating the kinetic parameters of molecular interactions such as protein protein and protein nucleic acid Where historically such measurements were made indirectly or by chemically modifying one or all of the interactants thus introducing the potential for altering the natural kinetic characteristics of the interactants a technique is now available that can measure these parameters less intrusively And where drug design discovery relies on understanding structure function relationships between biomolecules results from Biacore systems complement structural studies with detailed kinetic data utilizing relatively fast methodologies and consuming small amounts of precious reagents S C I E N T I F I C R E V I E W Pfizer purchased its first Biacore system to profile the kinetic characteristics of fusion proteins generated in several of its expression labs The application of the technology in other facets of the drug discovery process however quickly became apparent During the early 1990s our lab was charged with the development of peptide protein competition assays for three different therapeutic targets The format would be the same for the three assays the difference being the peptide and protein reagents An ELISA format was chosen to facilitate transfer to a high through put screen HTS The protocol utilized biotinylated target peptides bound via

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