The essential physiological process of converting the relatively inactive prohormone, thyroxine (T4), into the highly potent, biologically active hormone, triiodothyronine (T3), primarily through the action of specific deiodinase enzymes. This peripheral conversion is crucial because T3 is the primary ligand that binds to the nuclear thyroid hormone receptor, mediating nearly all of the hormone’s profound metabolic, cardiovascular, and developmental effects. Optimal activation is necessary for maintaining a state of euthyroid health.
Origin
The term is a descriptive phrase combining thyroid hormone, referring to the hormones produced by the thyroid gland, with activation, denoting the process of making a substance biologically functional and potent. This concept is fundamental to understanding thyroid physiology, recognizing that T4 is largely a circulating reservoir and T3 is the active, effector agent.
Mechanism
Thyroid hormone activation is catalyzed by the selenocysteine-containing deiodinase enzymes, specifically Type 1 (D1) and Type 2 (D2). D2 is the primary enzyme responsible for converting T4 to T3 in critical tissues like the brain and muscle, ensuring local T3 availability and action
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