Kinase Inhibitors: |
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Topic hints: |
Protein kinases are targets for treatment of a number of diseases. Kinase structures have informed drug design and have illuminated the mechanism of inhibition. In fact, they have provided insights into targeting the inactive or active form of the kinase, for targeting the global constellation of residues at the ATP site or less conserved additional pockets or single residues, and into targeting noncatalytic domains. Our laboratory works applying both direct structure-based drug design (SBDD) and indirect quantitative structure-activity relationship (QSAR) approaches to discover and optimize new potent and selective kinase inhibitors. Novel strategies for developing human Aurora A, protein kinase CK1 and CK2, MEK inhibitors such as virtual libraries design, high throughput docking, synthesis of parallel focused libraries and their biological screening are carrying out in our laboratories. |
Collaborators: |
Giorgio Cozza's group |
Pubblications: |