Update in TSH receptor agonists and antagonists

J Clin Endocrinol Metab. 2012 Dec;97(12):4287-92. doi: 10.1210/jc.2012-3080. Epub 2012 Sep 27.


The physiological role of the TSH receptor (TSHR) as a major regulator of thyroid function is well understood, but TSHRs are also expressed in multiple normal extrathyroidal tissues, and the physiological roles of TSHRs in these tissues are unclear. Moreover, TSHRs play a major role in several pathological conditions including hyperthyroidism, hypothyroidism, and thyroid tumors. Small molecule, "drug-like" TSHR agonists, neutral antagonists, and inverse agonists may be useful as probes of TSHR function in extrathyroidal tissues and as leads to develop drugs for several diseases of the thyroid. In this Update, we review the most recent findings regarding the development and use of these small molecule TSHR ligands.

Publication types

  • Research Support, N.I.H., Intramural
  • Review

MeSH terms

  • Animals
  • Antithyroid Agents / chemistry
  • Antithyroid Agents / pharmacology
  • Antithyroid Agents / therapeutic use
  • Drug Discovery / trends*
  • Endocrinology / trends
  • Hormone Antagonists / chemistry
  • Hormone Antagonists / pharmacology
  • Humans
  • Ligands
  • Models, Biological
  • Models, Molecular
  • Receptors, Thyrotropin / agonists*
  • Receptors, Thyrotropin / antagonists & inhibitors*
  • Receptors, Thyrotropin / chemistry
  • Receptors, Thyrotropin / physiology
  • Thyroid Diseases / drug therapy
  • Thyroid Diseases / etiology


  • Antithyroid Agents
  • Hormone Antagonists
  • Ligands
  • Receptors, Thyrotropin