Highly selective inhibition of IMPDH 2 provides the basis of antineuroinflammation therapy

@inproceedings{Liaoa2017HighlySI,
  title={Highly selective inhibition of IMPDH 2 provides the basis of antineuroinflammation therapy},
  author={Li-Xi Liaoa and Xiao-Min Songa and Li-Chao Wanga and Hai-Ning Lva and Jin-Feng Chena and Dan Liuc and Ge Fua and Ming-Bo Zhaoa and Yong Jianga and Ke-Wu Zenga and Peng-Fei Tua},
  year={2017}
}
  • Li-Xi Liaoa, Xiao-Min Songa, +8 authors Peng-Fei Tua
  • Published 2017
Inosine monophosphate dehydrogenase (IMPDH) of human is an attractive target for immunosuppressive agents. Currently, smallmolecule inhibitors do not show good selectivity for different IMPDH isoforms (IMPDH1 and IMPDH2), resulting in some adverse effects, which limit their use. Herein, we used a small-molecule probe specifically targeting IMPDH2 and identified Cysteine residue 140 (Cys140) as a selective druggable site. On covalently binding to Cys140, the probe exerts an allosteric regulation… CONTINUE READING
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