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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2010-12-17
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pubmed:abstractText |
Using an mGluR2 FRET-based binding assay, binders of the transmembrane region devoid of functional activity were identified. It is reported that slight chemical modifications of these SAMs can dramatically change activity of the resulting analogues without altering their affinities. Starting from compound 1, three mGluR2 NAMs showing also mGluR3 PAM activities were obtained. SAMs therefore represent a useful approach to explore the chemical space for GPCR allosteric modulator identification.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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|
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1520-4804
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pubmed:author |
|
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pubmed:issnType |
Electronic
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pubmed:day |
23
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
8775-9
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pubmed:meshHeading |
pubmed-meshheading:21105727-Allosteric Regulation,
pubmed-meshheading:21105727-Benzopyrans,
pubmed-meshheading:21105727-Calcium,
pubmed-meshheading:21105727-Cell Line,
pubmed-meshheading:21105727-Excitatory Amino Acid Agents,
pubmed-meshheading:21105727-Fluorescence Resonance Energy Transfer,
pubmed-meshheading:21105727-High-Throughput Screening Assays,
pubmed-meshheading:21105727-Humans,
pubmed-meshheading:21105727-Receptors, Metabotropic Glutamate,
pubmed-meshheading:21105727-Small Molecule Libraries,
pubmed-meshheading:21105727-Structure-Activity Relationship
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pubmed:year |
2010
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|
pubmed:articleTitle |
Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.
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pubmed:affiliation |
Domain Therapeutics SA, Bioparc, Boulevard Sebastien Brant, F-67400 Strasbourg-Illkirch, France. sschann@domaintherapeutics
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pubmed:publicationType |
Journal Article
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