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The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors
- Berndt, Alex;
- Miller, Simon;
- Williams, Olusegun;
- Le, Daniel D;
- Houseman, Benjamin T;
- Pacold, Joseph I;
- Gorrec, Fabrice;
- Hon, Wai-Ching;
- Ren, Pingda;
- Liu, Yi;
- Rommel, Christian;
- Gaillard, Pascale;
- Rückle, Thomas;
- Schwarz, Matthias K;
- Shokat, Kevan M;
- Shaw, Jeffrey P;
- Williams, Roger L
Published Web Location
https://doi.org/10.1038/nchembio.293Abstract
Upregulation of PI(3)K signaling pathways is implicated in many diseases, and a number of inhibitors are currently in clinical development. The structure of a PI(3)Kδ kinase domain, along with co-complexes with a diverse range of inhibitors, reveals new insights into mechanisms of inhibition and suggests isoform-selective design strategies.
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