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Liver cancer

g-Secretase; notch 1 (NOTCH1)

Cell culture and mouse studies suggest antagonizing NOTCH1 could be useful for treating cholangiocellular carcinoma (CCC), a form of liver cancer. Human cell lines derived from CCC tumors and CCC tissues had high levels of NOTCH1 signaling compared with other tumor lines and normal tissue. In mice, transgenic expression of a constitutively active form of NOTCH1 led to CCC. Also in mice, a g-secretase inhibitor blocked activation of NOTCH1 and decreased CCC growth compared with vehicle. Next steps include further characterization of NOTCH1 activity in human CCC tumors and testing
anti-NOTCH1 mAbs in mouse models.
At least six companies have NOTCH1 mAbs or g-secretase inhibitors in preclinical or Phase I testing to treat various cancers.

SciBX 6(27); doi:10.1038/scibx.2013.681
Published online July 18, 2013

Unpatented; licensing status not applicable

Zender, S. et al. Cancer Cell; published online May 30, 2013;
Contact: Nisar P. Malek, Eberhard Karls University of Tuebingen,
Tuebingen, Germany