Thyroid hormones structure-activity relationship

Structure—Activity Relationships. In spite of the considerable synthetic and bioassay effort involved in estabhshing the thyromimetic potency of thyroid-hormone analogues, more than 100 compounds have been studied (Table 2). The main stmctural requirements for thyromimetic activity can be summarized as follows (6,12—16). 

The structure-activity relationships of thyroid hormones and related structural analogs have been studied using both qualitative and quantitative methods, including the Hansch correlation. The structural requirements for receptor binding, and therefore hormone activity, are ... 

Zumstein M. Development of a quantitative structure-activity relationship for the a/ 3 specificity of the human thyroid hormone receptor. M.Sc. thesis. University of Basel, Switzerland, 2005. 

The understanding of structure-activity relationships also enabled the development of synthetic T3 (liothyronine), the metabolically more active form of thyroid hormone with a much shorter duration of action. This is especially useful for patients with thyroid carcinoma who are to undergo radioiodine imaging and possible treatment. Because of a half-life of only 24 hours, liothyronine substitution enables timelier radioiodine imaging and treatment, and as a result, patients experience less symptomatic hypothyroidism. 

Jorgensen EC. Thyroid hormones and analogs II. Structure-activity relationships. In Li CH, ed. Hormonal Proteins and Peptides, vol 6. New York Academic Press, 1978 107-204. 

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