Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.

  title={Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.},
  author={Kevin Michael Foote and J. Willem M. Nissink and Thomas M. McGuire and Paul Turner and Sylvie Guichard and James W. T. Yates and Alan Y K Lau and Kevin Blades and Dan Heathcote and Rajesh Odedra and Gary Wilkinson and Zena Wilson and Christine M Wood and Philip J. Jewsbury},
  journal={Journal of medicinal chemistry},
  volume={61 22},
The kinase ataxia telangiectasia mutated and rad3 related (ATR) is a key regulator of the DNA-damage response and the apical kinase which orchestrates the cellular processes that repair stalled replication forks (replication stress) and associated DNA double-strand breaks. Inhibition of repair pathways mediated by ATR in a context where alternative pathways are less active is expected to aid clinical response by increasing replication stress. Here we describe the development of the clinical… Expand
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