Targeting the thyroid-stimulating hormone receptor with small molecule ligands and antibodies

Abstract

Introduction: The thyroid-stimulating hormone receptor (TSHR) is the essential molecule for thyroid growth and thyroid hormone production. Since it is also a key autoantigen in Graves’ disease and is involved in thyroid cancer pathophysiology, the targeting of the TSHR offers a logical model for disease control.

Areas covered: We review the structure and function of the TSHR and the progress in both small molecule ligands and TSHR antibodies for their therapeutic potential.

Expert opinion: Stabilization of a preferential conformation for the TSHR by allosteric ligands and TSHR antibodies with selective modulation of the signaling pathways is now possible. These tools may be the next generation of therapeutics for controlling the pathophysiological consequences mediated by the effects of the TSHR in the thyroid and other extrathyroidal tissues.

Keywords:

• autoantibodies
• glycoprotein-hormone receptor
• Graves’ disease
• small molecule ligands
• thyroid cancer
• thyroid-stimulating hormone receptor

Declaration of interest

The authors state no conflict of interest and have received no payment in preparation of this manuscript.

Notes

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