Role of ELA region in auto-activation of mutant KIT receptor: a molecular dynamics simulation insight

  title={Role of ELA region in auto-activation of mutant KIT receptor: a molecular dynamics simulation insight},
  author={R. Purohit},
  journal={Journal of Biomolecular Structure and Dynamics},
  pages={1033 - 1046}
  • R. Purohit
  • Published 2014
  • Medicine, Chemistry
  • Journal of Biomolecular Structure and Dynamics
  • KIT receptor is the prime target in gastrointestinal stromal tumor (GISTs) therapy. Second generation inhibitor, Sunitinib, binds to an inactivated conformation of KIT receptor and stabilizes it in order to prevent tumor formation. Here, we investigated the dynamic behavior of wild type and mutant D816H KIT receptor, and emphasized the extended A-loop (EAL) region (805–850) by conducting molecular dynamics simulation (∼100 ns). We analyzed different properties such as root mean square cutoff or… CONTINUE READING
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