title: Update in TSH receptor agonists and antagonists.
abstract: 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.
authors.affiliation: Laboratory of Endocrinology and Receptor Biology, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA. marving@intra.niddk.nih.gov
authors.forename: Marvin C
authors.initials: MC
authors.lastname: Gershengorn
authors.forename: Susanne
authors.initials: S
authors.lastname: Neumann
mesh_terms: D000818:Animals; D013956:Antithyroid Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D055808:Drug Discovery / Q000639:trends*; D004704:Endocrinology / Q000639:trends; D006727:Hormone Antagonists / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D008954:Models, Biological; D008958:Models, Molecular; D011989:Receptors, Thyrotropin / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology; D013959:Thyroid Diseases / Q000188:drug therapy / Q000209:etiology
chemical_list: D013956:Antithyroid Agents; D006727:Hormone Antagonists; D008024:Ligands; D011989:Receptors, Thyrotropin