Discovery of a novel class of AKT pleckstrin homology domain inhibitors.

  title={Discovery of a novel class of AKT pleckstrin homology domain inhibitors.},
  author={Daruka Mahadevan and Garth Powis and Eugene A. Mash and Benjamin E. George and Vijay M. Gokhale and Shuxing Zhang and Kishore Shakalya and Lei Du-Cuny and Margareta Berggren and Maha Abdelmoneim Mohamed Ali and Umasish Jana and Nathan T. Ihle and Sylvestor Moses and Chloe Franklin and Satya T Narayan and Nikhil V. Shirahatti and Emmanuelle J. Meuillet},
  journal={Molecular cancer therapeutics},
  volume={7 9},
AKT, a phospholipid-binding serine/threonine kinase, is a key component of the phosphoinositide 3-kinase cell survival signaling pathway that is aberrantly activated in many human cancers. Many attempts have been made to inhibit AKT; however, selectivity remains to be achieved. We have developed a novel strategy to inhibit AKT by targeting the pleckstrin homology (PH) domain. Using in silico library screening and interactive molecular docking, we have identified a novel class of non-lipid-based… CONTINUE READING
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