Human TSH receptor ligands as pharmacological probes with potential clinical application

This is the authors' abstract. We don't add key points for this paper.

The biologic role of thyroid-stimulating hormone (TSH; thyrotropin) as an activator (agonist) of the TSH receptor (TSHR) in the hypothalamic-pituitary-thyroid axis is well known and activation of TSHR by recombinant human TSH is used clinically in patients with thyroid cancer. TSHR ligands other than TSH could be used to probe TSHR biology in thyroidal and extrathyroidal tissues, and potentially be employed in patients. A number of different TSHR ligands have been reported, including TSH analogs, antibodies and small-molecule, drug-like compounds. In this review, we will provide an update on all these classes of TSHR agonists and antagonists but place emphasis on small-molecule ligands.