Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

@article{Molina2013MonitoringDT,
  title={Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay},
  author={Daniel Martinez Molina and Rozbeh Jafari and Marina Ignatushchenko and Takahiro Seki and E. Andreas Larsson and Chen Dan and Lekshmy Sreekumar and Yihai Cao and P{\"a}r Nordlund},
  journal={Science},
  year={2013},
  volume={341},
  pages={84 - 87}
}
Drug Targeting Drug efficacy depends on the extent of binding to a cellular target (often a protein) with adverse effects caused by excessive target binding or by off-target binding. Engagement of a target protein inside cells is influenced by the effective drug concentration and by factors that regulate the protein conformation, making it difficult to predict efficacy based on in vitro affinity studies. Martinez Molina et al. (p. 84) took advantage of the shift in protein thermal stability… Expand
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