CRYSTALLIZED HUMAN XENOBIOTIC NUCLEAR RECEPTOR PXR/SXR LIGAND BINDING DOMAIN POLYPEPTIDE AND SCREENING METHODS EMPLOYING SAME

摘要

A solved three-dimensional crystal structure of a human PXR ligand binding domain polypeptide is disclosed, along with a crystal form of the PXR ligand binding domain. Orientations of the ligand SR12813 in the binding cavity are also disclosed. Additionally, methods of designing modulators of the biological activity of PXR, and other PXR ligand binding domain polypeptides, are also disclosed.