Corpus ID: 207857513

The characterization of idelalisib binding to PI 3 K δ 1 Structural , biochemical and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase delta *

@inproceedings{Somoza2015TheCO,
  title={The characterization of idelalisib binding to PI 3 K $\delta$ 1 Structural , biochemical and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase delta *},
  author={J. R. Somoza and David Koditek and Armando G. Villase and Nor and N. Novikov and Melanie H. Wong and Albert C Liclican and Weimei Xing and L. Lagpacan and Ruth Wang and B. Schultz and Giuseppe A. Papalia and D. Samuel and L. Lad and M. Mcgrath},
  year={2015}
}
Idelalisib (also known as GS-1101, CAL101, IC489666 and Zydelig) is a phosphoinositide 3-kinase delta (PI3Kδ) inhibitor that has recently been approved for the treatment of several hematological malignancies. Given its use in human diseases, we needed a clear picture of how idelalisib binds to and inhibits PI3Kδ . Our data show that idelalisib is a potent and selective inhibitor of the kinase activity of PI3Kδ . A kinetic characterization clearly demonstrated ATP-competitive inhibition, and… Expand

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