Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice.

@article{Neumann2009SmallmoleculeAF,
  title={Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice.},
  author={Susanne Neumann and Wenwei Huang and Steve R. Titus and Gerd Krause and Gunnar Kleinau and Anna Teresa Alberobello and Wei Zheng and Noel T Southall and James Inglese and Christopher P. Austin and Francesco Saverio Celi and Oksana Gavrilova and Craig J. Thomas and Bruce M. Raaka and Marvin C Gershengorn},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2009},
  volume={106 30},
  pages={12471-6}
}
Seven-transmembrane-spanning receptors (7TMRs) are prominent drug targets. However, small-molecule ligands for 7-transmembrane-spanning receptors for which the natural ligands are large, heterodimeric glycoprotein hormones, like thyroid-stimulating hormone (TSH; thyrotropin), have only recently been reported, and none are approved for human use. We have used quantitative high-throughput screening to identify a small-molecule TSH receptor (TSHR) agonist that was modified to produce a second… CONTINUE READING
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