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Review ArticleReview Article

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 and Douglas J. Kojetin
Dianne M. Perez, ASSOCIATE EDITOR
Pharmacological Reviews April 2013, 65 (2) 710-778; DOI: https://doi.org/10.1124/pr.112.006833
Thomas P. Burris
The Scripps Research Institute, Jupiter, Florida
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Laura A. Solt
The Scripps Research Institute, Jupiter, Florida
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Yongjun Wang
The Scripps Research Institute, Jupiter, Florida
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Christine Crumbley
The Scripps Research Institute, Jupiter, Florida
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Subhashis Banerjee
The Scripps Research Institute, Jupiter, Florida
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Kristine Griffett
The Scripps Research Institute, Jupiter, Florida
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Thomas Lundasen
The Scripps Research Institute, Jupiter, Florida
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Travis Hughes
The Scripps Research Institute, Jupiter, Florida
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Douglas J. Kojetin
The Scripps Research Institute, Jupiter, Florida
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Dianne M. Perez
The Scripps Research Institute, Jupiter, Florida
Roles: ASSOCIATE EDITOR
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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 ligand-binding 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.

Footnotes

  • dx.doi.org/10.1124/pr.112.006833.

  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 65 (2)
Pharmacological Reviews
Vol. 65, Issue 2
1 Apr 2013
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Review ArticleReview Article

Nuclear Receptors and Their Selective Modulators

Thomas P. Burris, Laura A. Solt, Yongjun Wang, Christine Crumbley, Subhashis Banerjee, Kristine Griffett, Thomas Lundasen, Travis Hughes and Douglas J. Kojetin
Pharmacological Reviews April 1, 2013, 65 (2) 710-778; DOI: https://doi.org/10.1124/pr.112.006833

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Review ArticleReview Article

Nuclear Receptors and Their Selective Modulators

Thomas P. Burris, Laura A. Solt, Yongjun Wang, Christine Crumbley, Subhashis Banerjee, Kristine Griffett, Thomas Lundasen, Travis Hughes and Douglas J. Kojetin
Pharmacological Reviews April 1, 2013, 65 (2) 710-778; DOI: https://doi.org/10.1124/pr.112.006833
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  • Article
    • Abstract
    • I. Introduction
    • II. Selective Estrogen Receptor Modulators
    • III. Vitamin D Receptor Modulators
    • IV. Thyroid Hormone Receptor Modulators
    • V. Selective Androgen Receptor Modulators
    • VI. Selective Glucocorticoid Receptor Modulators
    • VII. Selective Peroxisome Proliferator-Activated Receptor γ Modulators
    • VIII. Liver X Receptor Modulators
    • IX. Selective Progesterone Receptor Modulators
    • Authorship Contributions
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