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- W12355438 abstract "Publisher Summary This chapter reviews the literature on gonadotropin ligands upto 2005 and new literature on compound classes and biological data that has appeared during the past 3–4 years. The discovery of low-molecular-weight (LMW) agonists for G-protein-coupled receptors (GPCRs) that are normally activated by large proteins has met with limited success. Non-peptide antagonists for peptide-binding GPCRs are more often documented in literature. However, their optimization into suitable drug candidates has proven to be a challenging task. Several factors are responsible for this, the most important of which is the difficulty in reducing lipophilicity while retaining potency. The relatively high lipophilicity reflects the assumed binding mode of these non-peptide ligands. Whereas the endogenous ligand is known to bind to the large extracellular domain of the receptor, which is hydrophilic in nature, LMW compounds are believed to bind to the lipophilic transmembrane domain of the receptor. Strategies employing screening of large chemical libraries and subsequent hit and lead optimization have resulted in the identification of new chemical entities that mimic or modulate the activity of endogenous gonadotropins." @default.
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- W12355438 date "2009-01-01" @default.
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- W12355438 title "Chapter 8 Non-Peptide Ligands for the Gonadotropin Receptors" @default.
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