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Mutagenesis and Molecular Modeling of the Orthosteric Binding Site of the mGlu2 Receptor Determining Interactions of the Group II Receptor Antagonist 3H‐HYDIA |
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| Authors: | Linda Lundström Dr Bernd Kuhn Dr Jennifer Beck Edilio Borroni Dr Joseph?G Wettstein Dr Thomas?J Woltering Dr Silvia Gatti Dr |
| Affiliation: | Pharmaceutical Division, Discovery Research CNS and Medicinal Chemistry, F. Hoffmann‐La Roche Ltd., 4070 Basel (Switzerland), Fax: (+41)?61?6880382 |
| Abstract: | Binding of the mGlu2/3 antagonist HYDIA in the closed conformation model of mGlu2 causes repulsive interactions with Y216 in lobe II of the binding pocket, preventing closure of the VFT.  |
| Keywords: | HYDIA LY354740 metabotropic glutamate receptor mGlu2 molecular modeling mutagenesis |