Target intelligence / Profile preview

Thyroid-stimulating hormone (TSH)

Target
TSH
Molecular classification
Hormone, Glycoprotein hormone, Member of the cystine-knot growth factor superfamily, Anterior pituitary hormone
01

Overview

Thyroid-stimulating hormone (TSH) is a glycoprotein hormone produced by the anterior pituitary gland, primarily responsible for regulating the production and release of thyroid hormones thyroxine (T4) and triiodothyronine (T3) by stimulating the TSH receptor (TSHR) on thyroid follicular cells. It consists of two non-covalently linked subunits, alpha and beta, where the alpha subunit is common to similar hormones and the beta subunit confers specificity. Release of TSH is stimulated by thyrotropin-releasing hormone (TRH) from the hypothalamus, and inhibited by circulating thyroid hormones via a negative feedback loop. TSH levels serve as a sensitive clinical biomarker of thyroid axis integrity and are involved in disease states including hypothyroidism, hyperthyroidism, and autoimmune thyroid disorders such as Graves’ disease. TSH is itself not a receptor but acts via a specific G protein-coupled receptor (TSHR), making it an important target for therapies affecting thyroid function.

Other names
thyrotropinthyrotrophinTSH
02

Mechanism of action

Drugs may increase (hormone replacement) or decrease (antithyroid agents) circulating T4/T3, thus changing feedback on TSH secretion. Antithyroid drugs reduce thyroid hormone synthesis, increasing TSH through feedback. Hormone replacement lowers TSH by restoring negative feedback.

03

Biological functions

Regulation of thyroid hormone secretionModulation of metabolic ratePromotion of thyroid growth and developmentProtection of thyroid cells from apoptosisControl of heart and digestive functions, muscle control, brain development, and bone activity via thyroid hormone stimulation
04

Disease associations

HypothyroidismHyperthyroidismGraves' diseaseCongenital hypothyroidismGoiterOther thyroid dysfunctions
05

Safety considerations

Over-suppression or excessive stimulation leading to hypo- or hyperthyroidismCardiovascular complications due to altered metabolismBone density changes with long-term alteration of TSH/thyroid hormone axisDifficulty in accurate measurement due to TSH glycoform variability
06

Interacting drugs

Levothyroxine (thyroid hormone replacement)

4 more in the full profile.

07

Biomarkers

Serum TSH (routine biomarker for thyroid function)TSH glycoforms (for certain disorders and newborn screening)

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