Evolution of promiscuous nuclear hormone receptors: LXR, FXR, VDR, PXR, and CAR

  • Matthew D. Krasowski, Ai Ni, Lee R. Hagey, Sean Ekins
  • Molecular and Cellular Endocrinology, March 2011, Elsevier
  • DOI: 10.1016/j.mce.2010.06.016

evolution of LXR, FXR, VDR, PXR and CAR

What is it about?

This review describes the evolution of the LXR, FXR, VDR, PXR and CAR nuclear hormone receptors. These are key transcription factors that regulate gene expression. Ligands for these receptors cover a whole array of endogenous and exogenous compounds and there is extensive overlap in the ligand selectivity as well as transcriptional regulation networks. We have used an array of computational and experimental approaches to probe the evolution of these receptors.

Why is it important?

These nuclear receptors are important for regulating drug metabolizing enzymes and transporters and therefore impact exposure of drugs. Many of these receptors are quite flexible and therefore are quite promiscuous. We have proposed using a ligand based modeling approach to understand evolution across species.

Perspectives

Dr Sean Ekins
Collaborations in Chemistry

Over several years in collaboration with Dr. Matt Krasowski we worked on multiple nuclear receptors and generated computational models with the data produced by his lab. This review basically pulls all of this prior work together and interprets it as a whole. A fascinating body of work to be involved in creating.

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http://dx.doi.org/10.1016/j.mce.2010.06.016

The following have contributed to this page: Dr Sean Ekins