Searchable abstracts of presentations at key conferences in endocrinology
Endocrine Abstracts (2012) 29 S26.1

ICEECE2012 Symposia TSH Receptor (3 abstracts)

Low molecular weight antagonists of the TSH receptor

M. Gershengorn & S. Neumann

NIH, Bethesda, Maryland, USA.

Over the last several years, we have generated low molecular weight (LMW) antagonists of the TSH receptor (TSHR) that have the potential to be developed as drugs to treat patients with Graves’ hyperthyroidism (GD)/Graves’ ophthalmopathy (GO) and thyroid cancer. As GD is caused by persistent, unregulated activation of TSHRs by thyroid-stimulating antibodies (TSAbs) on thyrocytes and GO may be caused by activation of TSHRs on retro-orbital fibroblasts, a LMW TSHR antagonist could be used to treat GD and GO. Some antagonists, termed inverse agonists, in addition to inhibiting receptor stimulation by agonists like TSH and TSAbs, inhibit basal receptor signaling. As TSHR exhibits basal signaling, inverse agonists could be used to inhibit basal TSHR signaling on thyroid cancer cells and thereby further suppress activation of residual thyroid cancer. In this presentation, we will describe the data we have developed concerning the effects of these LMW antagonists in model cell systems over-expressing TSHRs, in primary cultures of human thyrocytes, and in primary cultures of fibroblasts from the retro-orbital space of patients with GO.

Declaration of interest: The authors declare that there is no conflict of interest that could be perceived as prejudicing the impartiality of the research project.

Funding: This work was supported, however funding details are unavailable.

Volume 29

15th International & 14th European Congress of Endocrinology

European Society of Endocrinology 

Browse other volumes

Article tools

My recent searches

No recent searches.

My recently viewed abstracts