Novel Compounds for Treatment of PI3K-Delta Mediated Diseases

University of California System: University of California, San Francisco
posted on 12/21/2009

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BACKGROUND:  In recent years, protein kinase inhibitors have become an important focus of development for targeted drug therapies, especially in cancer indications. A lot of current research focuses on phospho-inositol-3 Kinase (PI3K) inhibitors, as it is known that PI3 kinases mediate a very large number of autoimmune diseases and cancers. Given that different PI3K isoforms mediate different classes of diseases, the potential therapeutic value of PI3K inhibitors can be increased exponentially when their selectivity is tailored to a particular PI3 kinase isoform. Although many PI3K inhibitors are now available, none with specificity to particular isoforms exist.    TECHNOLOGY:   Our inventors have developed quite small and extremely potent PI3K antagonists with a strong specificity to the delta isoform of PI3 kinase. Furthermore, these novel compounds have a significantly lower molecular weight than the average comparable drug lead, resulting in a molecule with much greater overall drug efficiency.