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Structural, biochemical, and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase ?.

ABSTRACT: Idelalisib (also known as GS-1101, CAL-101, IC489666, and Zydelig) is a PI3K? 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 PI3K?. Our data show that idelalisib is a potent and selective inhibitor of the kinase activity of PI3K?. A kinetic characterization clearly demonstrated ATP-competitive inhibition, and several additional biochemical and biophysical assays showed that the compound binds reversibly and noncovalently to the kinase. A crystal structure of idelalisib bound to the p110? subunit of PI3K? furthers our understanding of the binding interactions that confer the potency and selectivity of idelalisib.

SUBMITTER: Somoza JR 

PROVIDER: S-EPMC4375495 | biostudies-literature | 2015 Mar

REPOSITORIES: biostudies-literature

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Structural, biochemical, and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase δ.

Somoza John R JR   Koditek David D   Villaseñor Armando G AG   Novikov Nikolai N   Wong Melanie H MH   Liclican Albert A   Xing Weimei W   Lagpacan Leanna L   Wang Ruth R   Schultz Brian E BE   Papalia Giuseppe A GA   Samuel Dharmaraj D   Lad Latesh L   McGrath Mary E ME  

The Journal of biological chemistry 20150128 13

Idelalisib (also known as GS-1101, CAL-101, IC489666, and Zydelig) is a 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 several additional biochemical and bio  ...[more]

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