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Brain cancer

Epidermal growth factor receptor (EGFR); Janus kinase-2 (JAK-2); PTEN (MMAC1; TEP1)

In vitro and mouse studies suggest allosteric inhibition of JAK-2 could help treat glioblastoma multiforme (GBM). In PTEN-deficient glioblastoma cell lines with constitutively active EGFR, compared with normal neural progenitor cells and astrocytes, the small molecule G5-7 selectively decreased proliferation. In vitro assays revealed that G5-7 bound to and allosterically inhibited JAK-2. In subcutaneous and intracranial xenograft mouse models of GBM, G5-7 decreased tumor growth compared with vehicle. Next steps include elucidating G5-7's mechanism of action and optimizing the compound for clinical development.
Incyte Corp. and Novartis AG market Jakafi ruxolitinib, a JAK-1 and JAK-2 inhibitor, to treat myeloproliferative disorder.
At least nine companies have JAK-2 inhibitors in Phase III testing or earlier development for various indications.

SciBX 6(34); doi:10.1038/scibx.2013.917
Published online Sept. 5, 2013

Patented by Emory University; licensed to Advinus Therapeutics Ltd.

He, K. et al. Sci. Signal.;
published online July 9, 2013;
Contact: Keqiang Ye,
Emory University School of Medicine, Atlanta, Ga.