Evolution of pharmacologic specificity in the pregnane X receptor |
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| Authors: | Sean Ekins Erica J Reschly Lee R Hagey Matthew D Krasowski |
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| Institution: | (1) Collaborations in Chemistry, Inc., Jenkintown, PA, USA;(2) Department of Pharmaceutical Sciences, University of Maryland, Baltimore, MD, USA;(3) Department of Pharmacology, University of Medicine and Dentistry of New Jersey, Robert Wood Johnson Medical School, Piscataway, NJ, USA;(4) Department of Pathology, University of Pittsburgh, Pittsburgh, PA, USA;(5) Department of Medicine, University of California at San Diego, San Diego, CA, USA |
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| Abstract: | Background The pregnane X receptor (PXR) shows the highest degree of cross-species sequence diversity of any of the vertebrate nuclear
hormone receptors. In this study, we determined the pharmacophores for activation of human, mouse, rat, rabbit, chicken, and
zebrafish PXRs, using a common set of sixteen ligands. In addition, we compared in detail the selectivity of human and zebrafish
PXRs for steroidal compounds and xenobiotics. The ligand activation properties of the Western clawed frog (Xenopus tropicalis) PXR and that of a putative vitamin D receptor (VDR)/PXR cloned in this study from the chordate invertebrate sea squirt (Ciona intestinalis) were also investigated. |
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