RT Journal Article
SR Electronic
T1 Nuclear Receptors and Their Selective Pharmacologic Modulators
JF Pharmacological Reviews
JO Pharmacol Rev
FD American Society for Pharmacology and Experimental Therapeutics
SP 710
OP 778
DO 10.1124/pr.112.006833
VO 65
IS 2
A1 Thomas P. Burris
A1 Laura A. Solt
A1 Yongjun Wang
A1 Christine Crumbley
A1 Subhashis Banerjee
A1 Kristine Griffett
A1 Thomas Lundasen
A1 Travis Hughes
A1 Douglas J. Kojetin
A2 Dianne M. Perez
YR 2013
UL http://pharmrev.aspetjournals.org/content/65/2/710.abstract
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.