Combining properties of different classes of PI3K{alpha} inhibitors to understand the molecular features that confer selectivity

In conclusion, we have used a structure-based design approach to combine features from two different compound classes to create new PI3Kα-selective inhibitors. This provides new insights into the contribution of different chemical units and interactions with different parts of the active site to the selectivity and potency of PI3Kα inhibitors.

Source: Biochemical Journal - June 26, 2017 Category: Biochemistry Authors: Gong, G. Q., Kendall, J. D., Dickson, J. M. J., Rewcastle, G. W., Buchanan, C. M., Denny, W. A., Shepherd, P. R., Flanagan, J. U. Tags: Research Articles Source Type: research