Binding-Pocket and Lid-Region Substitutions Render Human STING Sensitive to the Species-Specific Drug DMXAA

@inproceedings{Gao2014BindingPocketAL,
  title={Binding-Pocket and Lid-Region Substitutions Render Human STING Sensitive to the Species-Specific Drug DMXAA},
  author={P. Gao and Thomas Zillinger and Weiyi Wang and Manuel Ascano and Peihong Dai and Gunther Hartmann and Thomas Tuschl and Liang Deng and Winfried Barchet and Dinshaw J. Patel},
  booktitle={Cell reports},
  year={2014}
}
The drug DMXAA (5,6-dimethylxanthenone-4-acetic acid) showed therapeutic promise against solid tumors in mouse models but subsequently failed in human clinical trials. DMXAA was later discovered to activate mouse, but not human, STING, an adaptor protein in the cyclic dinucleotide cGAMP-mediated signaling pathway, inducing type I interferon expression. To facilitate the development of compounds that target human STING, we combined structural, biophysical, and cellular assays to study mouse and… CONTINUE READING
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