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Mar 1, 2009 (Vol. 29, No. 5)

TechNote: High-Throughput Kinase Selectivity Profiling

Bridging the Gulf between Compound Libraries and Rapid Discovery

  • Protein kinase-focused drug discovery efforts are escalating rapidly as research continues to elucidate and define the role of kinases in a growing list of diseases. To date, these research efforts have yielded eight FDA-approved small molecule kinase inhibitors with over 500 more in active development. While kinase inhibitors demonstrate great promise for disease treatment and management, target selectivity is a common challenge in drug development. 

    High-throughput screening in kinase inhibitor discovery is an effective platform for hit identification, compound annotation, and selectivity profiling. In the traditional kinase inhibitor discovery paradigm, however, a compound library is typically interrogated against a single kinase.

    The disadvantage with this approach is that it may overlook off-target interactions that may be important for understanding biological activity. Additionally, only a limited view of a library’s kinome-wide inhibition potential is provided, which may prevent identification of other therapeutically relevant interactions. 

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Scientifically Studying Ecstasy

MDMA (commonly known as the empathogen “ecstasy”) is classified as a Schedule 1 drug, which is reserved for compounds with no accepted medical use and a high abuse potential. Two researchers from Stanford, however, call for a rigorous scientific exploration of MDMA's effects to identify precisely how the drug works, the data from which could be used to develop therapeutic compounds.

Do you agree that ecstasy should be studied for its potential therapeutic benefits?

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