The role of protein and lipid kinases in cellular physiology and normal and abnormal growth has been well appreciated and has been the focus of intensive research in both academic arenas and pharmaceutical industries. The payoff for the pharmaceutical industries has been substantial.
Biochemical kinase profiling using a large panel of kinases with a broad coverage of the human kinome has become the de facto norm within the Pharma industry. The importance of this activity is demonstrated by the large number of service providers offering outsourced kinase profiling services.
EGFR ligands are a family of proteins which are involved in the regulation of cell growth and differentiation and their over-expression is associated with a number of cancers, including breast, lung and colon cancer. These ligands are expressed on the cell surface and include proteins such as epidermal growth factor (EGF), heparin binding EGF (HB-EGF) and transforming growth factor ? (TGF?).
Libraries of siRNAs directed against predefined subsets of genes now offer the capacity to greatly accelerate and improve the quality of functional genomics based drug discovery by enabling a much more targeted approach that effectively integrates the discovery and validation of novel targets.
With little sign of a decline in Pharma interest in kinase targets, greater emphasis is now being directed towards kinase selectivity profiling. A recent industry market survey suggests that although the market for kinase primary screening reagents is estimated to grow at an annual rate of 15%, that for outsourced kinase profiling is expected to reach 49% by 2005.
Overall, the end user is spoilt for choice with the range of alternative offerings, methodologies and approaches currently available for kinase screening and profiling.