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Proteros Fragments, Axikin Reach Milestones in Drug-discovery and -development for COPD


This story originally ran on Feb. 25.

Proteros Fragments and Axikin Pharmaceuticals this week said they have reached "significant milestones" in their drug-discovery collaboration.

The two firms have made "rapid progress" in the discovery and characterization of distinct chemical entities toward a novel therapeutic target for chronic obstructive pulmonary disease, the companies said in a joint statement.

In the first phase of the partnership, Proteros Fragments, using its X-ray crystallography platform, solved a de novo X-ray crystallographic structure of a protein targeted by Axikin. The company also developed a selective assay and screened its proprietary library of about 20,000 distinct novel fragments.

The fragment screen revealed hits from a number of distinct different chemotypes that bind to the active site of the target protein, whose identity was not disclosed. Each of the chemotypes has been validated, the companies said, and the binding mode was determined by X-ray crystallography "to develop the most promising candidate for subsequent fragment evolution, lead finding, and optimization."

Their collaboration, forged last April, is to discover lead compounds for inflammatory diseases. Under the terms of the deal, Proteros Fragments, headquartered in Martinsried, Germany, will provide research aimed at generating candidate leads for inhibiting a novel proprietary target protein [See PM 04/02/09].

Proteros Fragments was founded in the summer of 2008 as a subsidiary of Proteros Biostructures and offers services centered on the discovery of fragment-based lead structures.

Axikin is based in San Diego.

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