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Background: Idelalisib is a PI3Kδ inhibitor used to treat hematological malignancies.Results: Idelalisib is selective, noncovalent, reversible, and ATP-competitive.Conclusion: The crystal structure helps explain the potency and selectivity of idelalisib. The biophysical and biochemical data clarify the details of the inhibitor's interactions with PI3Kδ.Significance: Its use in humans makes it important to understand how idelalisib inhibits PI3Kδ.

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Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These molecules can coordinate to two divalent metal ions in the RNase H active site. Inhibition of enzymatic activity was measured in a biochemical assay, but no antiviral effect was observed. Binding was demonstrated via a solid state structure of the isolated p15-Ec domain of HIV-1 RT showing inhibitor and two Mn(II) ions bound to the RNase H active site.

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