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      Co-operative binding assay for the characterization of mGlu 4 allosteric modulators

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          Abstract

          The interest in the role of metabotropic glutamate receptor 4 (mGlu 4) in CNS related disorders has increased the need for methods to investigate the binding of allosteric drug candidates. Our aim is to present the first fully characterized in vitro binding assay of mGlu 4 positive allosteric modulators (PAMs). Results suggest that mGlu 4 PAMs have characteristic co-operative binding with orthosteric glutamate, which offers a notable insight to the further development of mGlu 4 targeted therapies.

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          Author and article information

          Journal
          Journal ID (nlm-journal-id): 0236217
          Journal ID (pubmed-jr-id): 6077
          Journal ID (nlm-ta): Neuropharmacology
          Journal ID (iso-abbrev): Neuropharmacology
          Title: Neuropharmacology
          ISSN (Print): 0028-3908
          ISSN (Electronic): 1873-7064
          Publication date Nihms-submitted: 8 July 2015
          Publication date (Electronic): 27 May 2015
          Publication date (Print): October 2015
          Publication date PMC-release: 01 October 2016
          Volume: 97
          Pages: 142-148
          Affiliations
          [1 ] Athinoula A. Martinos Biomedical Imaging Center, Massachusetts General Hospital, Harvard Medical School, Boston, MA, USA
          [2 ] Division of Surgical Oncology, Massachusetts General Hospital, Harvard Medical School, Boston, MA, USA
          [3 ] Experimental Therapeutics and Molecular Imaging Laboratory, Neuroscience Center, Department of Neurology, Massachusetts General Hospital, Boston, MA, USA; Program in Neuroscience, Harvard Medical School, Boston, MA, USA
          Author notes
          [* ]Corresponding author: Tel.: (617) 726-3807; Fax: (617) 726-7422; abrownell@ 123456partners.org
          Article
          Accession ID: PMC4537392 Pmcid ID: PMC4537392 Pmc-uid ID: 4537392 Manuscript ID: nihpa705483
          DOI: 10.1016/j.neuropharm.2015.05.017
          PMC ID: 4537392
          PubMed ID: 26025660
          SO-VID: 13480624-4049-444e-b61b-185a3a27161e
          History
          Categories
          Subject: Article

          Keywords: Binding affinity,Metabotropic glutamate receptor,Parkinson disease,mGlu4
          Data availability:
          Keywords: Binding affinity, Metabotropic glutamate receptor, Parkinson disease, mGlu4

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