Activation of CiVDR/PXR
What is it about?
We examined ligand binding by a xenobiotic receptor ortholog (VDR/PXR) of the tunicate Ciona intestinalis. Natural and synthetic toxins were assessed for binding to this receptor in vitro. Natural toxins may have acted as selected agents in the molecular evolution of the xenobiotic receptor.
Why is it important?
Pharmacophores were generated using the ligands and biologiocal data generated for the CiVDR/PXR. The common feature models suggested 2 hydrophobic features and a hydrogen bond acceptor were common features in the activiators. This pharmacophore had been previously generated for 3 earlier described ligands. The suggestion is that adaptive evolution has occured to the toxins okadaic acid and pectenotoxin-2.
The following have contributed to this page: Dr Sean Ekins