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Thyroid Stimulating Hormone Receptor (TSHR)
- Target
- TSHR
- Molecular classification
- G protein-coupled receptor, GPCR, Glycoprotein hormone receptor, Class A GPCR
01
Overview
The thyroid stimulating hormone receptor (TSHR) is a membrane-bound G protein-coupled receptor primarily expressed on thyroid follicular cells. Upon binding to thyroid-stimulating hormone (TSH), it initiates signaling cascades that stimulate thyroid hormone synthesis and release. Mutations and autoantibodies targeting TSHR are implicated in thyroid disorders like Graves' disease and hypothyroidism. TSHR is therefore a significant therapeutic target for managing these conditions.
- Other names
- Thyrotropin Receptor
02
Mechanism of action
Agonists (e.g., TSH, stimulatory autoantibodies) bind to TSHR, activating G-protein signaling cascades, increasing cAMP levels, and stimulating thyroid hormone production. Antagonists (e.g., blocking autoantibodies, small molecule antagonists) prevent TSHR activation, inhibiting thyroid hormone production.
03
Biological functions
Signal transductionRegulation of thyroid hormone synthesisRegulation of thyroid gland growthRegulation of thyroid gland developmentIodide uptakeThyroglobulin synthesisIodinationEndocytosis and proteolysisThyroid peroxidase activityRegulation of seasonal reproduction
04
Disease associations
Graves' diseaseHyperthyroidismHypothyroidismCongenital hypothyroidism
05
Safety considerations
HyperthyroidismHypothyroidismPotential for off-target effects with small molecule modulators
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