Proteros and Axikin reach significant milestones with integrated drug discovery project
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Proteros fragments and Axikin Pharmaceuticals Inc. announced the achievement of significant milestones in their integrated drug discovery collaboration.
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.”
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