Axikin Pharmaceuticals

Proteros and Axikin reach significant milestones with integrated drug
discovery project

Martinsried, Germany, and San Diego, USA, February 22nd, 2010 — In January 2010, only nine months after having set up the collaboration, rapid progress has been made in discovering and characterizing distinct chemical entities towards a novel therapeutic target for chronic obstructive pulmonary disease (COPD), which lies in Axikin's research area of respiratory disorders. During this first phase of the collaboration, Proteros solved a de-novo x-ray crystallographic structure of the protein targeted by Axikin, utilising Proteros’ unique x-ray crystallography platform. Additionally, Proteros established a selective assay and screened its proprietary library of approximately 20.000 distinct novel fragments.

This fragment screen revealed hits from a number of distinctive different chemotypes that specifically bound to the active site of the target protein. Each of these chemotypes has been validated and the binding mode was determined by x-ray crystallography to develop the most promising candidate for subsequent fragment evolution, lead finding and optimization.

“This first phase of the integrated drug discovery collaboration with the ability to utilize structure-guided SAR, has progressed very rapidly, yielding significant results and information that will facilitate the eventual identification of innovative, therapeutically valuable lead candidates for our pipeline”, said Kevin B. Bacon, President and CSO of Axikin Pharmaceuticals, and he added: “This highly valuable collaboration and the work ongoing at Proteros are certainly contributing to the success of Axikin’s overall approach in addressing unmet medical needs in the respiratory area.”

About Axikin Pharmaceuticals Inc.:
Axikin Pharmaceuticals, Inc. is a privately held biopharmaceutical company focused exclusively on the development and commercialization of small molecule therapeutics for severe respiratory, inflammatory and autoimmune diseases such as asthma, chronic obstructive pulmonary disease (COPD), inflammatory dermatoses, inflammatory bowel disease and rheumatoid arthritis. Axikin was spun out from Actimis Pharmaceuticals, in June 2008. Investors include Sanderling Ventures and Mitsui & Co. Venture Partners.

About Proteros fragments GmbH:
Proteros is a privately held company, which provides services and proprietary technologies to support integrated drug discovery within life sciences. The company accelerates and improves protein structure analysis and structure-based drug discovery by its expertise, industrialized processes and unique technologies for crystallography and fragment-based lead generation. Proteros complements its clients’ internal capabilities with external expertise and access to flexible resources. Proteros currently provides services for more than 60 pharmaceutical and biotechnology companies in North America, Europe and Japan.

Proteros fragments GmbH
Kurt Herrenknecht, Ph.D

Am Klopferspitz 19
82152 Martinsried
Phone: +49 (0) 89 7007 61 - 0
Fax. +49 (0) 89 7007 61 - 15

Axikin Pharmaceuticals Inc.
Kevin Bacon, Ph.D.

6185 Cornerstone Ct., Suite 106
San Diego, CA 92121
Phone:+1 (858) 458 - 1890
Fax: +1 (858) 642 - 6962



Media Contact
Karen Sparks

858-455-5500 x275

Company Contact
Kevin Bacon, Ph.D.
6185 Cornerstone Ct.
Suite 106
San Diego, CA 92121
Phone: (858) 458-1890


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