Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor.

@article{Nylander2012HumanTV,
  title={Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor.},
  author={Sven Nylander and Bj{\"o}rn Kull and J A Bj{\"o}rkman and J C Ulvinge and Nicholas D. Oakes and B M Emanuelsson and Maria L. E. Andersson and T V Ch Sk{\"a}rby and Tord Inghardt and Ola Fjellstr{\"o}m and David Gustafsson},
  journal={Journal of thrombosis and haemostasis : JTH},
  year={2012},
  volume={10 10},
  pages={2127-36}
}
BACKGROUND Based on in vitro and animal data, PI3Kβ is given an important role in platelet adhesion and aggregation but its role in insulin signaling is unclear. OBJECTIVE To strengthen the PI3Kβ target validation using the novel, short-acting inhibitor AZD6482. METHODS AND RESULTS AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm). A maximal anti-platelet effect was achieved at 1 μm in the in vitro and ex vivo tests both in dog and in man. In dog, in vivo… CONTINUE READING
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