AI Article Synopsis
- - A new inhibitor of the PI3Kδ enzyme is introduced, showing over 200 times more selectivity for other PI3K isoforms and additional kinases.
- - The selectivity is explained using structure-activity relationships and detailed crystal structures of the inhibitor bound to a specific mutant form of PI3Kγ.
- - Pharmacokinetic studies in rats and mice indicate that this inhibitor could be a valuable tool for in vivo research.
Article Abstract
A potent inhibitor of PI3Kδ that is ≥ 200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for selectivity is illustrated through structure activity relationships and crystal structures of compounds bound to a K802T mutant of PI3Kγ. Pharmacokinetic data in rats and mice support the use of 3 as a useful tool compound to use for in vivo studies.
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| http://dx.doi.org/10.1016/j.bmcl.2012.05.027 | DOI Listing |
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