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Discovery of Selective Luteinizing Hormone Receptor Agonists Using the Bivalent Ligand Method |
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| Authors: | Kimberly M. Bonger Dr. Richard J. B. H. N. van den Berg Dr. Annemiek D. Knijnenburg Laura H. Heitman Dr. Chris J. van Koppen Dr. Cornelis M. Timmers Dr. Herman S. Overkleeft Prof. Dr. Gijsbert A. van der Marel Prof. Dr. |
| Affiliation: | 1. Leiden Institute of Chemistry, Department of Bio‐Organic Synthesis, Gorlaeus Laboratories, Leiden University, PO Box 9502, 2300 RA Leiden (The Netherlands), Fax: (+31)?71‐5274307;2. Division of Medicinal Chemistry, LACDR, Leiden University, PO Box 9502, 2300 RA Leiden (The Netherlands);3. Department of Molecular Pharmacology, Schering‐Plough Research Institute, PO Box 20, 5340 BH Oss (The Netherlands);4. Department of Medicinal Chemistry, Schering‐Plough Research Institute, PO Box 20, 5340 BH Oss (The Netherlands) |
| Abstract: | Two series of dimeric ligands for a G‐protein‐coupled receptor were prepared that differ by the interconnecting spacer system. Biological evaluation revealed that both dimeric series exhibit unique biological properties relative to their monomeric counterparts.  |
| Keywords: | medicinal chemistry membrane proteins receptors signal transduction structure– activity relationships |