Drug, Discovery, and Development, July 5, 2007 Kinases are one of the most important classes of protein in cells. They play a role in cellular signaling, regulating everything from cell growth to inflammation. But, more importantly, when their function goes awry, kinases have been implicated in certain human cancers. Because of this role in cancer, kinases have been on the priority list that drug companies draw up while looking for new drug targets for years. Kinomics is a fairly new science. It basically relies on high-throughput screening assays to study the entire kinome (collection of all kinases in the cell) rapidly and accurately. But how this new science is being used differs from researcher to researcher. And, of course, the technologies they use also differ.  It seems like a rational credo would be that the more one knows about the biology of a kinase, the easier it will be to design a drug against it. And here's a case-in-point proving that this credo is indeed rational. "Designing drugs to interact with kinases might be more surgical than to design them to disrupt the global down-regulation of a gene, which can have wider off-target or side effects," says Norbert Herzog, PhD, associate professor of pathology at the University of Texas Medical Branch, Galveston, Texas. He explains that there would be less off-target effects if the inhibitor interacts with a single, specific kinase. And having the ability to design an inhibitor to block the function of a single kinase requires a deep understanding of that kinase's function-in other words-its biology.