Cellzome Technology Used to Unravel Novel Regulatory Mechanism in Cancer Signaling Pathway

September 16, 2009

HEIDELBERG, Germany, September 16 /PRNewswire/ –

– Integrated Chemical Genetics and Proteomics Approach Identifies new
Potential Drug Targets in Wnt Pathway

Cellzome announces today, the publication entitled “Tankyrase inhibition
stabilizes axin and antagonizes Wnt signalling”** is now available online in

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(TM) which we use for the
discovery and development of a new generation of kinase inhibitors and
Episphere(TM) for the discovery of novel drug candidates for epigenetic

** Huang, S., et.al. “Tankyrase inhibition stabilizes axin and
antagonizes Wnt signalling”, Nature, 10.1038/nature08356, 2009.

About Cellzome Inc.

Cellzome is a privately-owned drug discovery and development company
identifying a new generation of kinase-targeted drugs to treat inflammatory
diseases. Its pipeline of small-molecule therapeutics is driven by
Kinobeads(TM), a proprietary technology for the screening and profiling of
kinase inhibitors in physiologically-relevant cells and tissues. The most
advanced program, targeting PI3K(gamma), is anticipated to enter the clinic
in 2010, and several other programs are in early preclinical testing.

Cellzome is expanding its distinctive technology, in a novel form called
Episphere(TM), to the discovery and development of novel drug candidates for
epigenetic targets in their protein complexes.

Cellzome has significant collaborations with GSK and Johnson & Johnson.
Its holding company is domiciled in the US and it employs about 90 people at
its two laboratories in Cambridge, UK and Heidelberg, Germany.

SOURCE Cellzome Inc.

Source: newswire

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