Update in TSH Receptor Agonists and Antagonists | Zendy

Marvin C. Gershengorn | Zendy; Susanne Neumann | Zendy

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Update in TSH Receptor Agonists and Antagonists

Author(s) -

Marvin C. Gershengorn,

Susanne Neumann

Publication year - 2012

Publication title -

the journal of clinical endocrinology and metabolism

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.206

H-Index - 353

eISSN - 1945-7197

pISSN - 0021-972X

DOI - 10.1210/jc.2012-3080

Subject(s) - inverse agonist , thyrotropin receptor , receptor , pathological , regulator , thyroid , endocrinology , medicine , function (biology) , thyroid function , pharmacology , chemistry , neuroscience , agonist , biology , graves' disease , microbiology and biotechnology , biochemistry , gene

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.

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