Nuclear receptors and their selective pharmacologic modulators

Thomas P. Burris, Laura A. Solt, Yongjun Wang, Christine Crumbley, Subhashis Banerjee, Kristine Griffett, Thomas Lundasen, Travis Hughes, Douglas J. Kojetin

Research output: Contribution to journalReview article

104 Scopus citations

Abstract

Nuclear receptors are ligand-activated transcription factors and include the receptors for steroid hormones, lipophilic vitamins, sterols, and bile acids. These receptors serve as targets for development of myriad drugs that target a range of disorders. Classically defined ligands that bind to the ligandbinding domain of nuclear receptors, whether they are endogenous or synthetic, either activate receptor activity (agonists) or block activation (antagonists) and due to the ability to alter activity of the receptors are often termed receptor "modulators." The complex pharmacology of nuclear receptors has provided a class of ligands distinct from these simple modulators where ligands display agonist/partial agonist/antagonist function in a tissue or gene selective manner. This class of ligands is defined as selective modulators. Here, we review the development and pharmacology of a range of selective nuclear receptor modulators.

Original languageEnglish (US)
Pages (from-to)710-778
Number of pages69
JournalPharmacological Reviews
Volume65
Issue number2
DOIs
StatePublished - Jan 1 2013

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ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

Cite this

Burris, T. P., Solt, L. A., Wang, Y., Crumbley, C., Banerjee, S., Griffett, K., Lundasen, T., Hughes, T., & Kojetin, D. J. (2013). Nuclear receptors and their selective pharmacologic modulators. Pharmacological Reviews, 65(2), 710-778. https://doi.org/10.1124/pr.112.006833