Cellzome announces today, the publication entitled “Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling” is now available online in Nature. The paper describes how Cellzome’s quantitative chemical proteomics platform was used to identify a small molecule which plays a critical role in the regulation of the Wnt pathway.
The small molecule stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. Thus, the study provides new mechanistic insights into the regulation of axin protein homeostasis and presents new avenues for therapeutic intervention in this key cancer pathway. This transforming science was conducted as part of the collaboration between Cellzome and Novartis Institutes for Biomedical Research (NIBR)).Dr. David Simmons, CSO of Cellzome, said: “This paper shows the powerful insights provided by Cellzome’s proprietary chemical proteomics technology platform. Our platform also includes Kinobeads™ which we use for the discovery and development of a new generation of kinase inhibitors and Episphere™ for the discovery of novel drug candidates for epigenetic targets.”
Literature:Huang, S., et.al. "Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling", Nature, 10.1038/nature08356, 2009.