The NR superfamily comprises 48 transcription factors in humans that control a plethora of
gene network programs involved in a wide range of physiologic processes. This review will …

19F NMR has emerged as a powerful tool in drug discovery, particularly in fragment-based
screens. The favorable magnetic resonance properties of the fluorine-19 nucleus, the …

The lipid-sensing transcription factor PPARγ is the target of antidiabetic thiazolidinediones
(TZD). At two sites within its ligand binding domain, it also binds oxidized vitamin E …

Nuclear receptor (NR) transcription factors use a conserved activation function-2 (AF-2) helix
12 mechanism for agonist-induced coactivator interaction and NR transcriptional activation …

Efforts to decrease the adverse effects of nuclear receptor (NR) drugs have yielded
experimental agonists that produce better outcomes in mice. Some of these agonists have …

Binding of different ligands to glucocorticoid receptor (GR) may induce different
conformational changes and even trigger completely opposite biological functions. To …

Endocrine-disrupting chemicals (EDCs) can inadvertently interact with 12 classic nuclear
receptors (NRs) that disrupt the endocrine system and cause adverse effects. There is no …

Medicinal cannabis has remarkable therapeutic potential, but its clinical use is limited by the
psychotropic activity of Δ9-tetrahydrocannabinol (Δ9-THC). However, the biological profile of …

Small chemical modifications can have significant effects on ligand efficacy and receptor
activity, but the underlying structural mechanisms can be difficult to predict from static crystal …

The upregulation of PPARγ/RXRα transcriptional activity has emerged as a key event in
luminal bladder tumors. It renders tumor cell growth PPARγ-dependent and modulates the …