Kinases have become a proven target class for new drugs and have created a thirst for the development of new technology platforms for inhibitor detection. We discuss some of the latest technologies and techniques along with their advantages and disadvantages.
The human kinome comprises 518 known protein kinases and more than 20 lipid kinases. Nearly all aspects of control within a cell are modulated by reversible phosphorylation of proteins, mediated by protein kinases.
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.
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.