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  • Modulating Thyroid Hormones: Advances in TRb-Selective Ligands, Enzyme Inhibitors, and Deiodinase Mimetics for Endocrine Regulation

  • 1B. Pharm at Sandip Institute of Pharmaceuticals Sciences, Mahiravani Nashik Maharashtra 422213
    2M. Pharm at Sandip Institute of Pharmaceuticals Sciences Mahiravani Nashik Maharashtra 422213
     

Abstract

Thyroid hormones (THs) are critical regulators of metabolic homeostasis, influencing a wide array of physiological processes such as protein synthesis, lipid metabolism, neural development, skeletal maturation, and cardiovascular and renal functions. This review provides a comprehensive overview of thyroid hormone biosynthesis, activation, and the molecular mechanisms underlying their action via thyroid hormone receptors (TRs), with an emphasis on the TR? subtype.We delve into the therapeutic landscape of thyroid hormone analogues and emerging drug candidates—specifically, TR?-selective ligands and enzyme inhibitors—that target thyroid peroxidase and iodothyronine deiodinases for managing thyroid-related disorders. Special focus is given to the recent advancements in the design and function of small-molecule deiodinase mimetics, which offer promising avenues for precisely modulating thyroid hormone activity and levels in pathological conditions. This review aims to bridge basic endocrine science with translational pharmaceutical approaches, offering insights into novel therapeutic strategies and future directions in the management of thyroid dysfunctions.

Keywords

Hyperthyroidism, Graves’ disease, Methimazole, Propylthiouracil, carbimazole, Thyroid gland, Triiodothyronine, Calcitonin.

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Shreya Ingle
Corresponding author

B. Pharm at Sandip Institute of Pharmaceuticals Sciences, Mahiravani Nashik Maharashtra 422213

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Sunil Gaikwad
Co-author

M. Pharm at Sandip Institute of Pharmaceuticals Sciences Mahiravani Nashik Maharashtra 422213

Shreya Ingle*, Sunil Gaikwad, Modulating Thyroid Hormones: Advances in TR?-Selective Ligands, Enzyme Inhibitors, and Deiodinase Mimetics for Endocrine Regulation, Int. J. of Pharm. Sci., 2025, Vol 3, Issue 1, 726-742 https://doi.org/10.5281/zenodo.15273323

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