Thursday, September 5, 2013
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Epidermal growth factor receptor (EGFR);
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.
Corp. and Novartis
AG market Jakafi
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.
Published online Sept. 5, 2013
Patented by Emory
University; licensed to Advinus
He, K. et al. Sci.
published online July 9, 2013;
Contact: Keqiang Ye,
Emory University School of Medicine, Atlanta, Ga.
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