Proteros and Axikin Reach Milestone in Drug Discovery

Proteros fragments and Axikin Pharmaceuticals have announced the achievement of milestones in their integrated drug discovery collaboration.

In January 2010, progress has been made in discovering and characterizing distinct chemical entities towards a therapeutic target for Chronic Obstructive Pulmonary Disease (COPD), which lies in the latter’s research area of respiratory disorders.

During this first phase of the collaboration, the former solved a de-novo x-ray crystallographic structure of the protein that has been targeted by the latter, utilizing the former’s 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.