PT  - JOURNAL ARTICLE
AU  - Thomas P. Burris
AU  - Laura A. Solt
AU  - Yongjun Wang
AU  - Christine Crumbley
AU  - Subhashis Banerjee
AU  - Kristine Griffett
AU  - Thomas Lundasen
AU  - Travis Hughes
AU  - Douglas J. Kojetin
ED  - Perez, Dianne M.
TI  - Nuclear Receptors and Their Selective Pharmacologic Modulators
AID  - 10.1124/pr.112.006833
DP  - 2013 Apr 01
TA  - Pharmacological Reviews
PG  - 710--778
VI  - 65
IP  - 2
4099  - http://pharmrev.aspetjournals.org/content/65/2/710.short
4100  - http://pharmrev.aspetjournals.org/content/65/2/710.full
SO  - Pharmacol Rev2013 Apr 01; 65
AB  - 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.