Abstract:
The invention relates to chemical compounds that are useful in the treatment of a subject afflicted by a thyroid disease, in particular to compounds that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and their use in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
Abstract:
The invention relates to one or more regions of the thyroid-stimulating hormone receptor (TSHR), identified herein as a TSHR ligand binding domain. Such a domain is considered a binding pocket for chemical compounds, for example S37 or derivatives thereof, that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists. Embodiments of the invention relate to proteins and corresponding coding nucleic acids for the proteins of the invention, for example the TSHR ligand binding domain and related proteins. The invention relates to methods of screening for or testing compounds that interact, bind and/or modify the TSHR ligand binding domain of the invention.