Medical Letter on the CDC & FDA
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Life Sciences
Data on life sciences reported by S. Ekins and co-researchers
November 9th, 2008
"Very few antagonists have been identified for the human pregnane X receptor (PXR). These molecules may be of use for modulating the effects of therapeutic drugs, which are potent agonists for this receptor (e. g., some anticancer compounds and macrolide antibiotics), with subsequent effects on transcriptional regulation of xenobiotic metabolism and transporter genes," scientists in the United States report. "A recent novel pharmacophore for PXR antagonists was developed using three azoles and consisted of two hydrogen bond acceptor regions and two hydrophobic features. This pharmacophore also suggested an overall small binding site that was identified on the outer...
Source: Medical Letter on the CDC & FDA (2008-11-09)
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