Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor.

@article{Heitman2009SubstitutedTC,
  title={Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor.},
  author={Laura H Heitman and Rajeshwar Narlawar and Henk de Vries and Milou N Willemsen and Dieter R Wolfram and Johannes Brussee and Adriaan P. IJzerman},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 7},
  pages={2036-42}
}
The luteinizing hormone (LH) receptor plays an important role in fertility and certain cancers. The endogenous ligands human chorionic gonadotropin (hCG) and LH bind to the large N terminal domain of the receptor. We recently reported on the first radiolabeled low molecular weight (LMW) agonist for this receptor, [(3)H]Org 43553, which was now used to screen for new LMW ligands. We identified a terphenyl derivative that inhibited [(3)H]Org 43553 binding to the receptor, which led us to… CONTINUE READING

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