Dynamics of human protein kinase Aurora A linked to drug selectivity

@inproceedings{Pitsawong2018DynamicsOH,
  title={Dynamics of human protein kinase Aurora A linked to drug selectivity},
  author={Warintra Pitsawong and Vanessa Buosi and Renee Otten and Roman V. Agafonov and Adelajda Zorba and Nadja Kern and Steffen Kutter and Gunther Kern and Ricardo Ap P{\'a}dua and Xavier Meniche and Dorothee Kern},
  booktitle={eLife},
  year={2018}
}
Protein kinases are major drug targets, but the development of highly-selective inhibitors has been challenging due to the similarity of their active sites. The observation of distinct structural states of the fully-conserved Asp-Phe-Gly (DFG) loop has put the concept of conformational selection for the DFG-state at the center of kinase drug discovery. Recently, it was shown that Gleevec selectivity for the Tyr-kinase Abl was instead rooted in conformational changes after drug binding. Here, we… CONTINUE READING
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