Article
Tryptophan 299 is a conserved residue of human pregnane X receptor critical for the functional consequence of ligand binding.
Biochemical pharmacology - 15 Mar 2016
Banerjee Monimoy, Chai Sergio C, Wu Jing, Robbins Delira, Chen Taosheng
Abstract excerpt
PXR is a xenobiotic receptor that regulates drug metabolism by regulating the expression of drug-metabolizing enzymes including CYP3A4. It can be modulated by chemicals with different structures, functional groups and sizes. X-ray crystal structures of the ligand binding domain of human PXR (hPXR) alone or bound with agonists reveal a highly hydrophobic ligand binding pocket where the aromatic amino acid residue...
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