Enabling Protein Degradation Drug Discovery

Summer 2014: Targeted Chemical Libraries

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Although the widespread use of target-focused libraries has led to the rapid expansion of novel chemistry as research tools in drug discovery to exploit many classes of drug target, the ubiquitin system still remains a largely untapped medicinal chemistry opportunity. Protein kinases, on the other hand, have become one of the most important classes of drug targets for the pharmaceutical industry over the last decade, following on from the exploitation of kinase-focused libraries for at least the last two decades. Like protein phosphorylation by kinases, protein ubiquitylation regulates many aspects of cell function and provides a wealth of drug target opportunities across many therapeutic areas including cancer, cardiovascular, metabolism, inflammation, neurodegeneration and infectious diseases. In this article, we propose that chemical libraries which target the ubiquitin system are the missing keys to unlock the therapeutic potential of ubiquitin system drug discovery.

  • Summer 2014: Targeted Chemical Libraries
    'Targeted chemical libraries: the keys to unlock the ubiquitin system', an article by Jason Brown and J Mark Treherne published in Drug Discovery World.