THR
Thyroid hormone (TH aka triiodothyronine or T3) exerts a pleiotropic effect on development, differentiation, and metabolism through thyroid hormone receptors (TR or THR)[1]. In part because of associated hypercholesterolemia, hypothyroidism is associated with increased rates of atherosclerosis, while excessive levels of TH can lead to adverse effects, particularly in heart and bone. The beneficial metabolic effects of TH are mediated by the thyroid hormone receptor β isoform (THR-β, the predominant liver TH receptor), while the adverse heart and bone effects are primarily due to the interaction of TH with the THR-α[2].
[1] K Moriyama et al. Molecular characterization of human thyroid hormone receptor β isoform 4. Endocr Res. 2016;41(1):34-42.
[2] MJ Kelly et al. Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196). J Med Chem. 2014 May 22;57(10):3912-23.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2657 | MGL-3196 | Oral, liver-targeted, selective thyroid hormone receptor β-agonist | €90.00 | |
| 4126 | Sobetirome | High-affinity and selective thyroid hormone receptor β-agonist | €90.00 | |