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

…, R Narlawar, H de Vries, MN Willemsen…

Index: Heitman, Laura H.; Narlawar, Rajeshwar; De Vries, Henk; Willemsen, Milou N.; Wolfram, Dieter; Brussee, Johannes; IJzerman, Adriaan P. Journal of Medicinal Chemistry, 2009 , vol. 52, # 7 p. 2036 - 2042

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Citation Number: 26

Abstract

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,[3H] Org 43553, which was now used to screen for new LMW ligands. We identified a terphenyl derivative that inhibited [3H] Org 43553 ...