Hyperthyroidism (HyperT)

Hyperthyroidism is a clinical syndrome characterized by the excessive production and secretion of thyroid hormones, specifically thyroxine (T4) and triiodothyronine (T3), by the thyroid gland. It is a pathological condition rather than a single molecular target, frequently resulting from underlying diseases such as Graves' disease, toxic multinodular goiter, or toxic adenoma. In Graves' disease, the most common cause, the body produces autoantibodies that bind to and activate the thyroid-stimulating hormone receptor (TSHR), causing unregulated hormone synthesis. Current pharmacotherapy typically involves thionamides, such as methimazole and propylthiouracil, which inhibit the enzyme thyroid peroxidase (TPO) to block the organification of iodine. Other treatments include radioactive iodine therapy to ablate thyroid tissue or the use of beta-blockers to manage sympathomimetic symptoms like tachycardia. Because it describes a physiological state and disease entity, hyperthyroidism is not considered a valid molecular target name in drug discovery.

Other names

ThyrotoxicosisOveractive thyroidHyperthyreosisToxic diffuse goiter

Antithyroid drugs act as competitive inhibitors of the enzyme thyroid peroxidase (TPO), preventing the iodination of tyrosine residues on thyroglobulin. Radioactive iodine causes local tissue destruction of the thyroid follicles through beta-emission. Beta-blockers provide symptomatic relief by antagonizing beta-adrenergic receptors to counter the effects of excess thyroid hormone on the sympathetic nervous system.