A research team from SFI-CAST Innovation center at the Oslo University Hospital, led by Stefan Krauss, and including Jo Waaler, Daniel Holsworth, Andrew Voronkov and Jens Preben Morth have developed a highly selective tankyrase inhibitor. Tankyrase is a druggable target in the otherwise hard-to-hit Wnt signaling pathway and has implications in colon cancer, pancreas adenocarcinoma, ovary cancer, lung cancer and other solid tumors. The tankyrase inhibitor may open a new therapeutic approach.
Structural-relation activity data, crystallography and pharmacokinetics were reported in the Journal of Medicinal Chemistry while target validation data including mouse efficacy data, in collaboration with Roche's Genentech Inc. unit, were reported in Cancer Research. The work is highlighted as the cover story in SciBx, a weekly publication that unites the scientific acumen of the Nature Publishing Group with the business intelligence of BioCentury to provide analysis of the scientific content and commercial potential of the most important translational research papers with the potential to transform human therapeutics and diagnostics.
The Sci-Bx article's abstract page:
Analysis: Cover Story - Cancer
by Lev Osherovich, Senior Writer
SciBX 6(15); Published online April 18 2013
Articles mentioned in the text:
Voronkov A, Holsworth DD, Waaler J, Wilson SR, Ekblad B, Perdreau-Dahl H, Dinh H, Drewes G, Hopf C, Morth JP, Krauss S (2013)
Structural Basis and SAR for G007-LK, a Lead Stage 1,2,4-Triazole Based Specific Tankyrase 1/2 Inhibitor
J Med Chem, 56 (7), 3012-23
A Novel Tankyrase Small-molecule Inhibitor Suppresses APC Mutation-driven Colorectal Tumor Growth.
Lau T, Chan E, Callow M, Waaler J, Boggs J, Blake RA, Magnuson S, Sambrone A, Schutten M, Firestein R, Machon O, Korinek V, Choo E, Diaz D, Merchant M, Polakis P, Holsworth DD, Krauss S, Costa M.
Cancer Res. 2013 Mar 28.
Stefan Krauss home pages: