Table 3 Nuclear receptors can recognize and bind many ligands which have similar structures/patterns via its ligand-binding domain
Features of nuclear receptors’ ligand-binding domain | PMID |
|---|---|
1. Ligand-binding domains have the capacity to bind coactivator segments with LXXLL sequences, and corepressor segments with LXXXLXXX[I/L] sequences (where LÂ =Â leucine, IÂ =Â isoleucine, and XÂ =Â any amino acid) | 9808622 |
2. A single nuclear receptor controls the multitude of gene expressions | 20148675 |
3. The ligand-binding domain consists of a hydrophobic pocket that can bind a hydrophobic ligand | 20615454 |
4. Flexible ligands can contort to fit in the ligand-binding pocket | 9501913 |
5. Pharmacological antagonists and have been shown to bind to the receptor in the ligand-binding site and to inhibit hormone-activated receptor function | Â |
(1). NR1A1 ligand-binding domain can bind 3,5-dimethyl-3-isopropylthyronine except thyroid hormone | 8523397 |
(2). NR1B3 ligand-binding domain can bind to all-trans retinoic acid except vitamin A and related compounds | 7501014 |
(3). NR3A1 ligand-binding domain can bind to estradiol and raloxifene | 9338790 |