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Cellzome AG. (4/29/12). "Press Release: Cellzome Publishes in Nature Chemical Biology the Discovery of a Selective PI3Kg Inhibitor Driven by the Kinobeads Platform. Study Reveals PI3g Dependence of TH17 Cell Differentiation". Heidelberg.

Organisation Organisation Cellzome AG
  Group GlaxoSmithKline (GSK) (Group)
Products Product Kinobeads™ technology
  Product 2 PI3 kinase inhibitor

Cellzome scientists describe in an article published online in Nature Chemical Biology* today how a small molecule inhibitor identified with the Kinobeads™ screening and profiling platform was used to interrogate its anti-inflammatory function in human primary cell systems.

CZC24832 is the first selective PI3Kg inhibitor which is efficacious in in vitro and in vivo models of inflammation in rodents and humans and was designed using Kinobeads™. The scientists describe a new, so far undescribed role of PI3Kg in the regulation of TH17 cell differentiation, thus reinforcing selective inhibition of PI3Kg as a potential treatment for inflammatory and autoimmune diseases Kinobeads™ is Cellzome's technology for quantitatively measuring the extent that compounds or drugs interact with kinases within cells and tissues. Kinobeads™ work with native proteins and was used in this study to perform high throughput screening, to optimize potency and selectivity and to profile the activity of the compound against the entire kinome of different cells.

Gitte Neubauer, Vice President of Cellzome and senior author of the article said: "The publication demonstrates how powerful our approach to drug discovery is. We use native proteins in extracts of cultured and primary cells for a range of hemoproteomic experiments from library screening to in-depth profiling in different species. This allows good predictability of compound action in animal models and eventually in human clinical settings."

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About Cellzome

Cellzome is a world leader in chemoproteomics, transforming the sciences of epigenetics and signal transduction into novel drug candidates in inflammatory diseases and oncology. The Company maintains the highest levels of scientific expertise and has active collaborations with the foremost academic laboratories around the world. Cellzome's technologies work with native proteins in a physiological setting to discover
small molecule drugs targeting protein complexes that underlie diseases. The Company has a track record in delivering significant collaborations with top pharmaceutical companies including GlaxoSmithKline, Johnson & Johnson and Novartis. Cellzome is a privately-held, international, company located in Heidelberg, Germany and Cambridge, UK employing about 100 people. For more information please visit:

* Bergamini et al. A selective inhibitor reveals PI3Kg dependence of TH17 cell differentiation. Nature Chemical Biology. Published online: 29th April 2012, doi:10.1038/nchembio.957

Dr. Gitte Neubauer
Vice President of Research
Tel: +49 (0) 6221-137 57-100

Media contact:
Nicole Yost, Jayne Crook
College Hill
Tel: +44 (0)20 7866 7862

Cellzome AG Meyerhofstrasse 1, 69117 Heidelberg, Germany, Tel: +49 (0) 6221 137 57 0 Fax: +49 (0) 6221 137 57 201

Cellzome Limited Chesterford Research Park, Little Chesterford, Cambridge CB10 1XL, UK, Tel: +44 (0) 1799 532 800 Fax: +44 (0) 1799 532 801

Record changed: 2017-04-02


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